furans

Summary

Summary: Compounds with a 5-membered ring of four carbons and an oxygen. They are aromatic heterocycles. The reduced form is tetrahydrofuran.

Top Publications

  1. ncbi Small molecule RITA binds to p53, blocks p53-HDM-2 interaction and activates p53 function in tumors
    Natalia Issaeva
    Microbiology and Tumor Biology Center, Karolinska Institutet, SE 171 77 Stockholm, Sweden
    Nat Med 10:1321-8. 2004
  2. ncbi Inhibition of quorum sensing in Pseudomonas aeruginosa biofilm bacteria by a halogenated furanone compound
    Morten Hentzer
    Department of Molecular Microbiology, BioCentrum DTU, Technical University of Denmark, DK 2800 Lyngby, Denmark
    Microbiology 148:87-102. 2002
  3. ncbi HIPK2 regulation by MDM2 determines tumor cell response to the p53-reactivating drugs nutlin-3 and RITA
    Cinzia Rinaldo
    Department of Experimental Oncology, Molecular Oncogenesis Laboratory, Regina Elena Cancer Institute, Rome, Italy
    Cancer Res 69:6241-8. 2009
  4. ncbi Identification of arctigenin as an antitumor agent having the ability to eliminate the tolerance of cancer cells to nutrient starvation
    Suresh Awale
    Institute of Natural Medicine, Toyama Medical and Pharmaceutical University, Toyama, Japan
    Cancer Res 66:1751-7. 2006
  5. ncbi Rescue of the apoptotic-inducing function of mutant p53 by small molecule RITA
    Carolyn Y Zhao
    Department of Microbiology, Tumor and Cell Biology MTC, Karolinska Institutet, Stockholm, Sweden
    Cell Cycle 9:1847-55. 2010
  6. doi Ablation of key oncogenic pathways by RITA-reactivated p53 is required for efficient apoptosis
    Vera V Grinkevich
    Department of Microbiology, Tumor and Cell Biology, Karolinska Institutet, 17177, Stockholm, Sweden
    Cancer Cell 15:441-53. 2009
  7. pmc New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289
    Tanja Wenzler
    Department of Medical Parasitology and Infection Biology, Swiss Tropical Institute, Basel, Switzerland
    Antimicrob Agents Chemother 53:4185-92. 2009
  8. ncbi Induction of morphological and biochemical apoptosis following prolonged mitotic blockage by halichondrin B macrocyclic ketone analog E7389
    Galina Kuznetsov
    Department of Candidate Assessment and In Vitro Technologies, Eisai Research Institute, Andover, Massachusetts 01810, USA
    Cancer Res 64:5760-6. 2004
  9. pmc Furanone at subinhibitory concentrations enhances staphylococcal biofilm formation by luxS repression
    Richard Kuehl
    Division of Infection Biology, Department of Biomedicine, University Hospital Basel, Basel, Switzerland
    Antimicrob Agents Chemother 53:4159-66. 2009
  10. pmc A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat
    Michael F Jarvis
    Neuroscience Research, Abbott Laboratories, Abbott Park, IL 60064, USA
    Proc Natl Acad Sci U S A 104:8520-5. 2007

Detail Information

Publications355 found, 100 shown here

  1. ncbi Small molecule RITA binds to p53, blocks p53-HDM-2 interaction and activates p53 function in tumors
    Natalia Issaeva
    Microbiology and Tumor Biology Center, Karolinska Institutet, SE 171 77 Stockholm, Sweden
    Nat Med 10:1321-8. 2004
    ..RITA may serve as a lead compound for the development of an anticancer drug that targets tumors with wild-type p53...
  2. ncbi Inhibition of quorum sensing in Pseudomonas aeruginosa biofilm bacteria by a halogenated furanone compound
    Morten Hentzer
    Department of Molecular Microbiology, BioCentrum DTU, Technical University of Denmark, DK 2800 Lyngby, Denmark
    Microbiology 148:87-102. 2002
    ..It does, however, affect the architecture of the biofilm and enhances the process of bacterial detachment, leading to a loss of bacterial biomass from the substratum...
  3. ncbi HIPK2 regulation by MDM2 determines tumor cell response to the p53-reactivating drugs nutlin-3 and RITA
    Cinzia Rinaldo
    Department of Experimental Oncology, Molecular Oncogenesis Laboratory, Regina Elena Cancer Institute, Rome, Italy
    Cancer Res 69:6241-8. 2009
    ..These data indicate that strategies of p53 reactivation by MDM2 inhibition should also take into consideration MDM2 targets other than p53, such as the apoptosis activator HIPK2...
  4. ncbi Identification of arctigenin as an antitumor agent having the ability to eliminate the tolerance of cancer cells to nutrient starvation
    Suresh Awale
    Institute of Natural Medicine, Toyama Medical and Pharmaceutical University, Toyama, Japan
    Cancer Res 66:1751-7. 2006
    ....
  5. ncbi Rescue of the apoptotic-inducing function of mutant p53 by small molecule RITA
    Carolyn Y Zhao
    Department of Microbiology, Tumor and Cell Biology MTC, Karolinska Institutet, Stockholm, Sweden
    Cell Cycle 9:1847-55. 2010
    ..Thus, RITA is a promising lead for the development of anti-cancer drugs that reactivate the tumor suppressor function of p53 in cancer cells irrespective whether they express mutant or wild type p53...
  6. doi Ablation of key oncogenic pathways by RITA-reactivated p53 is required for efficient apoptosis
    Vera V Grinkevich
    Department of Microbiology, Tumor and Cell Biology, Karolinska Institutet, 17177, Stockholm, Sweden
    Cancer Cell 15:441-53. 2009
    ..Inhibition of oncogenes by p53 reduces the cell's ability to buffer proapoptotic signals and elicits robust apoptosis. Our study highlights the role of transcriptional repression for p53-mediated tumor suppression...
  7. pmc New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289
    Tanja Wenzler
    Department of Medical Parasitology and Infection Biology, Swiss Tropical Institute, Basel, Switzerland
    Antimicrob Agents Chemother 53:4185-92. 2009
    ..In conclusion, DB868 with oral and DB829 with parenteral application are potential candidates for further development of a second-stage African sleeping sickness drug...
  8. ncbi Induction of morphological and biochemical apoptosis following prolonged mitotic blockage by halichondrin B macrocyclic ketone analog E7389
    Galina Kuznetsov
    Department of Candidate Assessment and In Vitro Technologies, Eisai Research Institute, Andover, Massachusetts 01810, USA
    Cancer Res 64:5760-6. 2004
    ..These results show that prolonged mitotic blockage by E7389 can lead to apoptotic cell death of human cancer cells in vitro and can provide a mechanistic basis for the significant in vivo anticancer efficacy of E7389...
  9. pmc Furanone at subinhibitory concentrations enhances staphylococcal biofilm formation by luxS repression
    Richard Kuehl
    Division of Infection Biology, Department of Biomedicine, University Hospital Basel, Basel, Switzerland
    Antimicrob Agents Chemother 53:4159-66. 2009
    ..In summary, we observed a biofilm enhancement by furanone in staphylococci at subinhibitory concentrations, which was manifested by an increase in PIA and dependent on luxS...
  10. pmc A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat
    Michael F Jarvis
    Neuroscience Research, Abbott Laboratories, Abbott Park, IL 60064, USA
    Proc Natl Acad Sci U S A 104:8520-5. 2007
    ..These data demonstrate that acute and selective pharmacological blockade of Na(v)1.8 sodium channels in vivo produces significant antinociception in animal models of neuropathic and inflammatory pain...
  11. doi Synthesis and antitumor activity of 2,5-bis(3'-indolyl)-furans and 3,5-bis(3'-indolyl)-isoxazoles, nortopsentin analogues
    Patrizia Diana
    Dipartimento Farmacochimico, Tossicologico e Biologico, Universita degli Studi di Palermo, Via Archirafi 32, 90123 Palermo, Italy
    Bioorg Med Chem 18:4524-9. 2010
    A series of novel 2,5-bis(3'-indolyl)furans and 3,5-bis(3'-indolyl)isoxazoles were synthesized as antitumor agents. The antiproliferative activity was evaluated in vitro toward diverse human tumor cell lines...
  12. pmc Apparent half-lives of dioxins, furans, and polychlorinated biphenyls as a function of age, body fat, smoking status, and breast-feeding
    Meghan O Grady Milbrath
    Department of Environmental Health Sciences, University of Michigan School of Public Health, Ann Arbor, Michigan 48109 2029, USA
    Environ Health Perspect 117:417-25. 2009
    ....
  13. pmc Novel arylimidamides for treatment of visceral leishmaniasis
    Michael Zhuo Wang
    Eshelman School of Pharmacy, The University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA
    Antimicrob Agents Chemother 54:2507-16. 2010
    ....
  14. pmc Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment
    Denise da Gama Jaen Batista
    Laboratorio de Biologia Celular, Instituto Oswaldo Cruz, Fundacao Oswaldo Cruz, Rio de Janeiro, RJ, Brazil
    Antimicrob Agents Chemother 54:2940-52. 2010
    ..Our data clearly show the trypanocidal efficacy of DB766, suggesting that this AIA may represent a new lead compound candidate to Chagas' disease treatment...
  15. pmc YC-1 inhibited human platelet aggregation through NO-independent activation of soluble guanylate cyclase
    C C Wu
    Pharmacological Institute, College of Medicine, National Taiwan University, Taipei
    Br J Pharmacol 116:1973-8. 1995
    ..7. These results would suggest that YC-1 activates sGC of human platelets by a NO-dependent mechanism, and exerts its antiplatelet effects through the sGC/cyclic GMP pathway...
  16. ncbi Activity of "reversed" diamidines against Trypanosoma cruzi "in vitro"
    C F Silva
    Lab Biologia Celular, Instituto Oswaldo Cruz, FIOCRUZ, Rio de Janeiro, Brazil
    Biochem Pharmacol 73:1939-46. 2007
    ..Our results show the activity of reversed diamidines against T. cruzi and suggested that the compounds merit in vivo studies...
  17. ncbi Structural basis for the recognition of the FapydG lesion (2,6-diamino-4-hydroxy-5-formamidopyrimidine) by formamidopyrimidine-DNA glycosylase
    Franck Coste
    Centre de Biophysique Moleculaire, UPR4301, CNRS, rue Charles Sadron, 45071 Orleans Cedex 02, France
    J Biol Chem 279:44074-83. 2004
    ..The significant differences between the Fpg recognition modes of 8-oxodG and FapydG provide new insights into the Fpg substrate specificity...
  18. ncbi The primary antimitotic mechanism of action of the synthetic halichondrin E7389 is suppression of microtubule growth
    Mary Ann Jordan
    Molecular, Cellular, and Developmental Biology, University of California Santa Barbara, 93106 9610, USA
    Mol Cancer Ther 4:1086-95. 2005
    ..The result is formation of abnormal mitotic spindles that cannot pass the metaphase/anaphase checkpoint...
  19. pmc Inhibition of centromere dynamics by eribulin (E7389) during mitotic metaphase
    Tatiana Okouneva
    Department of Molecular, Cellular, and Developmental Biology and Neuroscience Research Institute, University of California Santa Barbara, Santa Barbara, CA 93106, USA
    Mol Cancer Ther 7:2003-11. 2008
    ..The strong correlation between suppression of kinetochore-microtubule dynamics and mitotic arrest indicates that the primary mechanism by which eribulin blocks mitosis is suppression of spindle microtubule dynamics...
  20. doi Phase I study of eribulin mesylate administered once every 21 days in patients with advanced solid tumors
    Antoinette R Tan
    The Cancer Institute of New Jersey, New Brunswick, New Jersey 08901, USA
    Clin Cancer Res 15:4213-9. 2009
    ..To evaluate the maximum tolerated dose (MTD), dose-limiting toxicities (DLT), and pharmacokinetics of eribulin mesylate (E7389), a halichondrin B analogue, administered every 21 days in patients with advanced solid tumors...
  21. ncbi PI-103, a dual inhibitor of Class IA phosphatidylinositide 3-kinase and mTOR, has antileukemic activity in AML
    S Park
    Institut Cochin, Universite Paris Descartes, CNRS UMR 8104, Paris, France
    Leukemia 22:1698-706. 2008
    ..Here, we demonstrate that multitargeted therapy against PI3K/Akt and mTOR with PI-103 may be of therapeutic value in AML...
  22. pmc Reverse transcriptase inhibitors as potential colorectal microbicides
    Carolina Herrera
    Division of Cellular and Molecular Medicine, St George s University of London, Cranmer Terrace, London SW17 0RE, United Kingdom
    Antimicrob Agents Chemother 53:1797-807. 2009
    ..These findings may have important implications for the rational design of effective rectal microbicides...
  23. ncbi Annonacin, a natural mitochondrial complex I inhibitor, causes tau pathology in cultured neurons
    Myriam Escobar-Khondiker
    Experimental Neurology, Philipps University, D 35033 Marburg, Germany
    J Neurosci 27:7827-37. 2007
    ....
  24. pmc Drugging the PI3 kinome: from chemical tools to drugs in the clinic
    Paul Workman
    Cancer Research UK Centre for Cancer Therapeutics, Section of Cancer Therapeutics, The Institute of Cancer Research, Haddow Laboratories, Sutton, Surrey, United Kingdom
    Cancer Res 70:2146-57. 2010
    ..The challenges and outlook for drugging the PI3 kinome are discussed in the more general context of the role of structural biology and chemical biology in innovative drug discovery...
  25. doi Norfuraneol dephosphorylates eNOS at threonine 495 and enhances eNOS activity in human endothelial cells
    Christoph A Schmitt
    Department of Pharmacognosy, University of Vienna, Althanstrasse 14, 1090 Vienna, Austria
    Cardiovasc Res 81:750-7. 2009
    ..The aim of this study was to show whether NF, which is taken up regularly, for example with cooked food, affects the human endothelial nitric oxide synthase (eNOS) system...
  26. pmc Attenuation of Pseudomonas aeruginosa virulence by quorum sensing inhibitors
    Morten Hentzer
    BioCentrum DTU, Technical University of Denmark, DK 2800 Lyngby, Denmark
    EMBO J 22:3803-15. 2003
    ..aeruginosa biofilms increased bacterial susceptibility to tobramycin and SDS. In a mouse pulmonary infection model, the drug inhibited quorum sensing of the infecting bacteria and promoted their clearance by the mouse immune response...
  27. ncbi In vitro metabolism of an orally active O-methyl amidoxime prodrug for the treatment of CNS trypanosomiasis
    J H Ansede
    Division of Drug Delivery and Disposition, School of Pharmacy, The University of North Carolina, Chapel Hill, NC 27599, USA
    Xenobiotica 35:211-26. 2005
    ..The active antitrypanosomal metabolite, DB820, was the last metabolite to be formed and thus provides evidence that DB844 may effectively be metabolized to its active metabolite in vivo...
  28. doi Mutated and non-mutated TP53 as targets in the treatment of leukaemia
    H Nahi
    Department of Haematology, Karolinska University Hospital at Huddinge, Stockholm, Sweden
    Br J Haematol 141:445-53. 2008
    ..In both AML and CLL cells exposure to RITA resulted in induction of intracellular p53. We conclude that small molecules targeting p53 might be of clinical importance in the future for treating drug-resistant leukaemia...
  29. ncbi Furanones as potential anti-bacterial coatings on biomaterials
    J K Baveja
    Cooperative Research Centre for Eye Research and Technology, University of New South Wales, Sydney, NSW 2052, Australia
    Biomaterials 25:5003-12. 2004
    ..Bacterial load on all furanone-coated materials was significantly reduced (p<0.001) as was slime production (p<0.001). There is a potential for furanone-coated biomaterials to be used to reduce medical device-associated infections...
  30. ncbi In vitro and in vivo anticancer activities of synthetic macrocyclic ketone analogues of halichondrin B
    M J Towle
    Department of Anticancer Research Eisai Research Institute. Andover, Massachusetts 01810, USA
    Cancer Res 61:1013-21. 2001
    ....
  31. doi Rescue of p53 function by small-molecule RITA in cervical carcinoma by blocking E6-mediated degradation
    Carolyn Ying Zhao
    Department of Microbiology, Tumor and Cell Biology, Karolinska Institutet, Stockholm, Sweden
    Cancer Res 70:3372-81. 2010
    ..These results provide a proof of principle for the treatment of cervical cancer in a p53-dependent manner by using small molecules that target p53...
  32. doi Pharmacological activation of the p53 pathway in haematological malignancies
    Manujendra N Saha
    Division of Cellular and Molecular Biology, Toronto General Hospital Research Institute, University of Toronto, Canada
    J Clin Pathol 63:204-9. 2010
    ..This review will highlight recent findings in the research into molecules capable of modulating p53 protein activities and mechanisms that activate the p53 pathway, restoring response to therapy in haematological malignancies...
  33. ncbi Effects of biomass hydrolysis by-products on oleaginous yeast Rhodosporidium toruloides
    Cuimin Hu
    Dalian Institute of Chemical Physics, Chinese Academy of Sciences, 457 Zhongshan Road, Dalian, PR China
    Bioresour Technol 100:4843-7. 2009
    ..Our work will be useful for optimization of biomass hydrolysis processes and lipid production using lignocellulosic materials...
  34. ncbi A selective Nav1.8 sodium channel blocker, A-803467 [5-(4-chlorophenyl-N-(3,5-dimethoxyphenyl)furan-2-carboxamide], attenuates spinal neuronal activity in neuropathic rats
    Steve McGaraughty
    Neuroscience Research, Abbott Laboratories, R4PM, AP9 1, 100 Abbott Park Rd, Abbott Park, IL 60064 6118, USA
    J Pharmacol Exp Ther 324:1204-11. 2008
    ..However, Na(v)1.8 sodium channels on central terminals seem to be key to the modulation of spontaneous firing in SNL rats...
  35. ncbi Arctigenin, a phenylpropanoid dibenzylbutyrolactone lignan, inhibits MAP kinases and AP-1 activation via potent MKK inhibition: the role in TNF-alpha inhibition
    Min Kyung Cho
    College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, Seoul 151 742, South Korea
    Int Immunopharmacol 4:1419-29. 2004
    ....
  36. ncbi Additive antinociceptive effects of the selective Nav1.8 blocker A-803467 and selective TRPV1 antagonists in rat inflammatory and neuropathic pain models
    S K Joshi
    Abbott Laboratories, Neuroscience Research, Abbott Park, Illinois, USA
    J Pain 10:306-15. 2009
    ..Using such a combination strategy to produce analgesia may potentially provide an improved therapeutic separation from unwanted in vivo side effects associated with blockade of either Nav1.8 or TRPV1 alone...
  37. doi The dual PI3K/mTOR inhibitor PI-103 promotes immunosuppression, in vivo tumor growth and increases survival of sorafenib-treated melanoma cells
    Marta López-Fauqued
    Medical Oncology Research Program, Vall d Hebron Research Institute, Vall d Hebron Institute of Oncology VHIO, Vall d Hebron Hospital, Barcelona 08035, Spain
    Int J Cancer 126:1549-61. 2010
    ..These data certainly makes an argument for investigating unexpected effects of rational drug combinations on immunocompetent animal models prior to conducting clinical studies...
  38. doi Highly cytotoxic and neurotoxic acetogenins of the Annonaceae: new putative biological targets of squamocin detected by activity-based protein profiling
    Séverine Derbré
    Laboratoire de Pharmacognosie associé au CNRS, UMR 8076, Faculte de Pharmacie, Universite Paris Sud 11, Chatenay Malabry Cedex, France
    Bioorg Med Chem Lett 18:5741-4. 2008
    ..These results give new insights into the mechanism of action of these potent neurotoxic molecules...
  39. ncbi Selective cytotoxicity of squamocin on T24 bladder cancer cells at the S-phase via a Bax-, Bad-, and caspase-3-related pathways
    Shyng Shiou F Yuan
    Department of Medical Research, E Da Hospital, I Shou University, Kaoshiung County, Taiwan 824, ROC
    Life Sci 78:869-74. 2006
    ..These results suggest that squamocin is a potentially promising anticancer compound...
  40. ncbi Highly favorable antiviral activity and resistance profile of the novel thiocarboxanilide pentenyloxy ether derivatives UC-781 and UC-82 as inhibitors of human immunodeficiency virus type 1 replication
    J Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Mol Pharmacol 50:394-401. 1996
    ....
  41. pmc Cembranoids with 3,14-ether linkage and a secocembrane with bistetrahydrofuran from the Dongsha Atoll soft coral Lobophytum sp
    Mohamed Elamir F Hegazy
    Department of Marine Biotechnology and Resources, National Sun Yat Sen University, Kaohsiung 804, Taiwan
    Mar Drugs 9:1243-53. 2011
    ..Among these metabolites, 1-4 are rarely found cembranoids possessing a tetrahydrofuran moiety with a 3,14-ether linkage. In addition, 5 is the first secocembrane possessing two tetrahydrofuran moieties with 3,14- and 4,7-ether linkages...
  42. doi Deregulation of Cdk2 causes Bim-mediated apoptosis in p53-deficient tumors following actin damage
    H D Chae
    National Research Laboratory, Department of Microbiology, Dankook University College of Medicine, Cheonan, Korea
    Oncogene 27:4115-21. 2008
    ..Therefore, these results suggest that Bim-mediated apoptosis following actin damage due to deregulation of Cdk2 and the cell cycle by the absence of functional p53...
  43. ncbi The pyridinylfuranopyrimidine inhibitor, PI-103, chemosensitizes glioblastoma cells for apoptosis by inhibiting DNA repair
    M A Westhoff
    University Children s Hospital, Ulm, Germany
    Oncogene 28:3586-96. 2009
    ....
  44. doi Differential inhibitory effects of inotilone on inflammatory mediators, inducible nitric oxide synthase and cyclooxygenase-2, in LPS-stimulated murine macrophage
    Yu Ching Kuo
    Department of Food Science, Rutgers University, New Brunswick, NJ, USA
    Mol Nutr Food Res 53:1386-95. 2009
    ..Our results suggest that inotilone may have potential to be developed into an effective anti-inflammatory agent...
  45. ncbi Molecular pharmacology of phosphatidylinositol 3-kinase inhibition in human glioma
    Sandrine Guillard
    Signal Transduction and Molecular Pharmacology Team, Cancer Research UK Centre for Cancer Therapeutics, The Institute of Cancer Research, Sutton, Surrey, UK
    Cell Cycle 8:443-53. 2009
    ..Our results support the therapeutic potential for PI3 kinase inhibitors with a PI-103-like profile as therapeutic agents for the treatment of glioma...
  46. pmc Preclinical safety assessments of UC781 anti-human immunodeficiency virus topical microbicide formulations
    D L Patton
    Department of Obstetrics and Gynecology, University of Washington, Seattle, WA 98195 6460, USA
    Antimicrob Agents Chemother 51:1608-15. 2007
    ..1% UC781 formulation. These results provide additional support for the continued development of UC781 formulations as anti-HIV microbicides...
  47. ncbi Therapeutic effect of arctiin and arctigenin in immunocompetent and immunocompromised mice infected with influenza A virus
    Kyoko Hayashi
    Graduate School of Medicine and Pharmaceutical Sciences for Research, University of Toyama, Sugitani, Toyama, Japan
    Biol Pharm Bull 33:1199-205. 2010
    ..Thus, monotherapy of arctiin or combined therapy of arctiin with oseltamivir would be another treatment option for influenza...
  48. ncbi Pectenotoxin-2 induces G2/M phase cell cycle arrest in human breast cancer cells via ATM and Chk1/2-mediated phosphorylation of cdc25C
    Dong Oh Moon
    Laboratory of Immunobiology, Department of Marine Life Sciences, Jeju National University, Jeju 690 756, Republic of Korea
    Oncol Rep 24:271-6. 2010
    ..We also observed that PTX-2-induced cell cycle arrest was not restricted to p53 status in human breast cancer cells...
  49. doi Delineation of the interactions between the chemotherapeutic agent eribulin mesylate (E7389) and human CYP3A4
    Z Y Zhang
    Department of Drug Disposition, Eisai Research Institute, 4 Corporate Drive, Andover, MA 01810, USA
    Cancer Chemother Pharmacol 62:707-16. 2008
    ....
  50. doi Furanones, potential agents for preventing Staphylococcus epidermidis biofilm infections?
    Jessica Lönn-Stensrud
    Department of Oral Biology, Faculty of Dentistry, University of Oslo, Oslo, Norway
    J Antimicrob Chemother 63:309-16. 2009
    ..The aim of the present study was to find furanones that decrease biofilm formation without irritative or genotoxic effects, or effects on S. epidermidis growth...
  51. doi In vitro anti-inflammatory effects of arctigenin, a lignan from Arctium lappa L., through inhibition on iNOS pathway
    Feng Zhao
    School of Pharmacy, Yantai University, Yantai, Shandong, China
    J Ethnopharmacol 122:457-62. 2009
    ..Compositae) which has been widely used as a Traditional Chinese Medicine for dispelling wind and heat included in Chinese Pharmacophere, was found to exhibit anti-inflammatory activities but its molecular mechanism remains unknown yet...
  52. ncbi Oocyte-based screening of cytokinesis inhibitors and identification of pectenotoxin-2 that induces Bim/Bax-mediated apoptosis in p53-deficient tumors
    Hee Don Chae
    National Research Laboratory, Department of Microbiology, Dankook University College of Medicine, Anseo 29, Cheonan 330 714, Korea
    Oncogene 24:4813-9. 2005
    ..Therefore, these results suggest that Bim triggers apoptosis by activating Bax in p53-deficient tumors upon actin damage, and that actin inhibitors may be potent chemotherapeutic agents against p53-deficient tumors...
  53. pmc Acceptability of UC781 gel as a rectal microbicide among HIV-uninfected women and men
    Ana Ventuneac
    HIV Center for Clinical and Behavioral Studies, New York State Psychiatric Institute and Columbia University, 1051 Riverside Drive, Unit 15, New York, NY 10032, USA
    AIDS Behav 14:618-28. 2010
    ..Acceptability research is essential in early phases of microbicide development to identify potential problems, understand user preferences, and introduce changes if needed...
  54. ncbi In vivo anti-inflammatory and antinociceptive effects of liriodendrin isolated from the stem bark of Acanthopanax senticosus
    Hyun Ju Jung
    Division of Applied Plant Sciences, Sangji University, Woosan Dong, Wonju, Korea
    Planta Med 69:610-6. 2003
    ..These results suggest that the anti-inflammatory and antinociceptive effects of liriodendrin after oral administration were attributable to the in vivo transformation to syringaresinol, which may function as the active constituent...
  55. ncbi Factors on the formation of disinfection by-products MX, DCA and TCA by chlorination of fulvic acid from lake sediments
    C Zhuo
    State Key Laboratory of Pollution Control and Resource Reuse, School of the Environment, Nanjing University, People's Republic of China
    Chemosphere 45:379-85. 2001
    ..Lower pH, longer time, greater chlorine dose can result in greater yield of both DCA and TCA, and there is a strong linear relationship between the formation of DCA and TCA...
  56. ncbi Ginkgolides and bilobalide: their physical, chromatographic and spectroscopic properties
    Teris A van Beek
    Laboratory of Organic Chemistry, Natural Products Chemistry Group, Wageningen University, Dreijenplein 8, 6703 HB Wageningen, The Netherlands
    Bioorg Med Chem 13:5001-12. 2005
    ..The literature until April 2005 has been reviewed...
  57. ncbi DABCO-catalyzed reaction of alpha-halo carbonyl compounds with dimethyl acetylenedicarboxylate: a novel method for the preparation of polysubstituted furans and highly functionalized 2H-pyrans
    Mingjin Fan
    State Key Laboratory of Applied Organic Chemistry, Lanzhou University, Lanzhou 730000, PR China
    J Org Chem 70:8204-7. 2005
    Chemical reaction: see text] Polysubstituted furans and highly functionalized 2H-pyrans were prepared in good yields by DABCO-catalyzed reactions of alpha-halo carbonyl compounds with dimethyl acetylenedicarboxylate (DMAD) at room ..
  58. ncbi Pharmacologic characterization of a potent inhibitor of class I phosphatidylinositide 3-kinases
    Florence I Raynaud
    Cancer Research UK Centre for Cancer Therapeutics, The Institute of Cancer Research, Haddow and McElwain Laboratories, Sutton, Surrey, United Kingdom
    Cancer Res 67:5840-50. 2007
    ....
  59. doi Novel diamidino-substituted derivatives of phenyl benzothiazolyl and dibenzothiazolyl furans and thiophenes: synthesis, antiproliferative and DNA binding properties
    Livio Racane
    Department of Applied Chemistry, Faculty of Textile Technology, University of Zagreb, Baruna Filipovića 28a 10000 Zagreb, Croatia
    J Med Chem 53:2418-32. 2010
    ..diisopropylamidino-, and diimidazolinyl-substituted derivatives of phenyl benzothiazolyl and dibenzothiazolyl furans and thiophenes were successfully prepared and evaluated for their antiproliferative activity on tumor cell lines ..
  60. doi A high-performance liquid chromatography-tandem mass spectrometry method for the clinical combination study of carboplatin and anti-tumor agent eribulin mesylate (E7389) in human plasma
    Christopher Desjardins
    Drug Safety and Disposition, Eisai Research Institute, 4 Corporate Drive, Andover, MA 01810, USA
    J Chromatogr B Analyt Technol Biomed Life Sci 875:373-82. 2008
    ..Both compounds were stable in human plasma (>or=80 days at -80 degrees C), at room temperature (>or=4h), following three freeze-thaw cycles and in 50/50 methanol/H(2)O (<4 degrees C for >or=252 days)...
  61. pmc Design, synthesis, and structure-activity relationship of a novel series of 2-aryl 5-(4-oxo-3-phenethyl-2-thioxothiazolidinylidenemethyl)furans as HIV-1 entry inhibitors
    Alan R Katritzky
    Department of Chemistry, Center for Heterocyclic Compounds, University of Florida, Gainesville, Florida 32611, USA
    J Med Chem 52:7631-9. 2009
    ..molecular docking analysis, we designed a series of 2-aryl 5-(4-oxo-3-phenethyl-2-thioxothiazolidinylidenemethyl)furans. Compared with 12 and 13, these compounds have bigger molecular size (437-515 Da) and could occupy more space in ..
  62. pmc Efficient glycosidation of a phenyl thiosialoside donor with diphenyl sulfoxide and triflic anhydride in dichloromethane
    David Crich
    Department of Chemistry, University of Illinois at Chicago, 845 West Taylor Street, Chicago, Illinois 60607 7061, USA
    Org Lett 8:959-62. 2006
    ..With an excess of diphenyl sulfoxide, glycal formation can be completely suppressed and excellent yields are obtained for coupling to a wide range of primary, secondary, and tertiary acceptors...
  63. ncbi Monitoring dioxins and furans in a population living near a hazardous waste incinerator: levels in breast milk
    M Schuhmacher
    Laboratory of Toxicology and Environmental Health, School of Medicine, Rovira i Virgili University, Calle San Lorenzo 21, 43201 Reus, Spain
    Chemosphere 57:43-9. 2004
    ..The results of the present study, as well as other recent environmental and biological data, indicate that living in the vicinity of this HWI should not mean additional health risks due to PCDD/PCDFs for the general population...
  64. pmc Small-molecule activation of p53 blocks hypoxia-inducible factor 1alpha and vascular endothelial growth factor expression in vivo and leads to tumor cell apoptosis in normoxia and hypoxia
    Jun Yang
    Cancer Research UK Centre for Cancer Therapeutics, The Institute of Cancer Research, Surrey, United Kingdom
    Mol Cell Biol 29:2243-53. 2009
    ..Through the identification of a new mechanism of action for RITA, our study uncovers a novel link between the DNA damage response-p53 pathway and the protein translational machinery...
  65. pmc Does long term residency near industry have an impact on the body burden of polychlorinated dibenzo-p-dioxins, furans, and polychlorinated biphenyls in older women?
    T Pless-Mulloli
    School of Population and Health Sciences, The Medical School, Newcastle upon Tyne, UK
    Occup Environ Med 62:895-901. 2005
    ..Polychlorinated dibenzo-dioxins and furans (PCDD/F) and polychlorinated biphenyls (PCBs) have been useful markers in some settings...
  66. ncbi Furanones
    R de Nys
    School of Marine Biology and Aquaculture, James Cook University, Townsville Q4811, Australia
    Prog Mol Subcell Biol 42:55-86. 2006
    ..This review summarises the extensive work on furanones focusing on their natural and applied antifouling activities...
  67. ncbi Antiviral treatment of calves persistently infected with bovine viral diarrhoea virus
    Benjamin W Newcomer
    Department of Clinical Sciences, College of Veterinary Medicine, Auburn University, Auburn, AL, USA
    Antivir Chem Chemother 22:171-9. 2012
    ..The purpose of this research was to initiate evaluation of the pharmacokinetic and safety data of a novel antiviral agent in BVDV-free calves and to assess the antiviral efficacy of the same agent in PI calves...
  68. pmc Detection of inhibition of bovine viral diarrhea virus by aromatic cationic molecules
    M Daniel Givens
    Department of Pathobiology, College of Veterinary Medicine, Auburn University, Auburn, Alabama 36849, USA
    Antimicrob Agents Chemother 47:2223-30. 2003
    ..The leading compounds require further investigation to determine their mechanism of action, in vivo activity, and specific activity against hepatitis C virus...
  69. doi In-depth search focused on furans, lactones, volatile phenols, and acetals as potential age markers of Madeira wines by comprehensive two-dimensional gas chromatography with time-of-flight mass spectrometry combined with solid phase microextraction
    Rosa Perestrelo
    QOPNA, Departamento de Química, Universidade de Aveiro, 3810 193 Aveiro, Portugal
    J Agric Food Chem 59:3186-204. 2011
    ..Considering the chemical groups of furans, lactones, volatile phenols, and acetals, 103 volatile compounds were tentatively identified; among these, 71 have ..
  70. ncbi Biological performance of a novel synthetic furanone-based antimicrobial
    J K Baveja
    Graduate School of Biomedical Engineering, University of New South Wales, Sydney NSW 2052, Australia
    Biomaterials 25:5013-21. 2004
    ..These results demonstrate negligible acute inflammatory response to synthetic brominated antibacterial furanones. Future studies will focus on chronic responses and examination of in vivo efficacy...
  71. pmc Direct inhibition of the DNA-binding activity of POU transcription factors Pit-1 and Brn-3 by selective binding of a phenyl-furan-benzimidazole dication
    Paul Peixoto
    INSERM U 837, Team 4 Molecular and cellular targeting for cancer treatment, Jean Pierre Aubert Research Center, Institut de Recherches sur le Cancer de Lille, Place de Verdun, F 59045 Lille, IMPRT IFR114, Lille, France
    Nucleic Acids Res 36:3341-53. 2008
    ..These findings are the first to show that heterocyclic dications can inhibit major groove transcription factors and they open the door to the control of transcription factors activity by those compounds...
  72. ncbi Inability of p53-reactivating compounds Nutlin-3 and RITA to overcome p53 resistance in tumor cells deficient in p53Ser46 phosphorylation
    Teng Ma
    Section of Molecular Embryology, Graduate School of Medical and Dental Sciences, Tokyo Medical and Dental University, Japan
    Biochem Biophys Res Commun 417:931-7. 2012
    ..Thus, the dysregulation of this phosphorylation in tumor cells may be a critical factor that limits the efficacy of these p53-based cancer therapies...
  73. ncbi Synthesis of furanone-based natural product analogues with quorum sensing antagonist activity
    Thomas Hjelmgaard
    Department of Chemistry, Organic Chemistry, Bld 201, Technical University of Denmark, DK 2800 Kgs Lyngby, Denmark
    Bioorg Med Chem 11:3261-71. 2003
    ..Although the synthesized compounds are not as potent quorum sensing inhibitors as some natural counterparts and a synthetic analogue hereof, interesting structure-activity relationships are seen...
  74. doi Design, synthesis, and biological activity of a novel series of 2,5-disubstituted furans/pyrroles as HIV-1 fusion inhibitors targeting gp41
    Shibo Jiang
    Lindsley F Kimball Research Institute, New York Blood Center, NY 10065, USA
    Bioorg Med Chem Lett 21:6895-8. 2011
    Based on molecular docking analysis of earlier results, we designed a series of 2,5-disubstituted furans/pyrroles (5a-h) as HIV-1 entry inhibitors...
  75. ncbi Prevention and elimination of bovine viral diarrhea virus infections in fetal fibroblast cells
    M Daniel Givens
    127 Sugg Laboratory, College of Veterinary Medicine, Auburn University, AL 36849 5516, USA
    Antiviral Res 64:113-8. 2004
    ..Our results demonstrate that in vitro infections with BVDV can be effectively prevented or eliminated by addition of aromatic cations...
  76. doi α-Glucosidase and aldose reductase inhibitory activities from the fruiting body of Phellinus merrillii
    Guan Jhong Huang
    School of Chinese Pharmaceutical Sciences and Chinese Medicine Resources, College of Pharmacy, China Medical University, Taichung, Taiwan
    J Agric Food Chem 59:5702-6. 2011
    ..The importance of finding effective antidiabetic therapeutics led us to further investigate natural compounds...
  77. ncbi Preclinical experience with two selective progesterone receptor modulators on breast and endometrium
    H J Kloosterboer
    Research and Development N V Organon, Oss, The Netherlands
    Steroids 65:733-40. 2000
    ..Ovulation is resumed shortly after stopping treatment, and a normal menses occurs after the first progesterone peak. Both compounds may be interesting options for the prevention and treatment of breast cancer and for fertility control...
  78. doi Transient PI3K inhibition induces apoptosis and overcomes HGF-mediated resistance to EGFR-TKIs in EGFR mutant lung cancer
    Ivan S Donev
    Division of Medical Oncology, Cancer Research Institute, Kanazawa University, Kanazawa, Japan
    Clin Cancer Res 17:2260-9. 2011
    ..The purpose of this study was to determine whether inhibition of PI3K, a downstream molecule of both EGFR and MET, could overcome HGF-mediated EGFR-TKI resistance in EGFR mutant lung cancer cells PC-9 and HCC827...
  79. pmc A structural basis for regulation of actin polymerization by pectenotoxins
    John S Allingham
    Department of Biochemistry, Queen s University, Kingston, Ontario, Canada K7L 3N6
    J Mol Biol 371:959-70. 2007
    ..Examination of the PTX-binding site on actin provides a rationalization for the structure-activity relationships observed in vivo and in vitro, and may provide a basis for predicting toxicity of PTX analogues...
  80. doi Pectenotoxin-2 represses telomerase activity in human leukemia cells through suppression of hTERT gene expression and Akt-dependent hTERT phosphorylation
    Mun Ock Kim
    Department of Microbiology, Pusan National University, Busan 609 735, Republic of Korea
    FEBS Lett 582:3263-9. 2008
    ..We concluded that PTX-2 suppressed telomerase activity through the transcriptional and post-translational suppression of hTERT and this process precedes cellular differentiation of human leukemia cells...
  81. ncbi Regiocontrolled intramolecular cyclizations of carboxylic acids to carbon-carbon triple bonds promoted by acid or base catalyst
    Masanobu Uchiyama
    Graduate School of Pharmaceutical Sciences, Tohoku University, Aoba ku, Sendai 980 8578, Japan
    Org Lett 8:5517-20. 2006
    ..Density functional theory calculations and application to a short route to thunberginol A were also described. [reaction: see text]...
  82. doi Two new compounds from the dried tender stems of Cinnamomum cassia
    Chao Liu
    Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, China
    J Asian Nat Prod Res 11:845-9. 2009
    ..7 microM. Compounds 3-8 were isolated from the title plant for the first time...
  83. ncbi Toxicity and carcinogenicity of furan in human diet
    Nadiya Bakhiya
    Department of Food Safety, Federal Institute for Risk Assessment, Berlin, Germany
    Arch Toxicol 84:563-78. 2010
    ..As this may give rise for concern, in this review, the currently available toxicological and mechanistic data of furan are summarized and discussed with regard to its applicability in assessing the risk of furan in human diet...
  84. ncbi Three new furan derivatives and a new fatty acid from a Taiwanese marine sponge Plakortis simplex
    Y C Shen
    Institute of Marine Resources, National Sun Yat Sen University, 70 Lien Hai Road, Kaohsiung, Taiwan, Republic of China
    J Nat Prod 64:324-7. 2001
    ..Biological studies revealed that compound 7 exhibited cytotoxic activity against COLO-250 and KB-16 cells, and compound 1 is active against KB-16 cells...
  85. ncbi Data requirements for risk assessment of furan in food
    C W Heppner
    European Food Safety Authority, Unit on Contaminants, Parma, Parma, Italy
    Food Addit Contam 24:114-21. 2007
    ..The European Food Safety Authority's (EFSA) Scientific Panel on Contaminants in the Food Chain (CONTAM) recommended these studies as part of a reliable risk assessment of furan in food...
  86. ncbi Induction of apoptosis by pectenotoxin-2 is mediated with the induction of DR4/DR5, Egr-1 and NAG-1, activation of caspases and modulation of the Bcl-2 family in p53-deficient Hep3B hepatocellular carcinoma cells
    Dong Yeok Shin
    Department of Biochemistry, Dongeui University College of Oriental Medicine, Busan 614 052, Korea
    Oncol Rep 19:517-26. 2008
    ....
  87. ncbi Pectenotoxin-2 abolishes constitutively activated NF-kappaB, leading to suppression of NF-kappaB related gene products and potentiation of apoptosis
    Mun Ock Kim
    Department of Microbiology, College of Natural Sciences, Pusan National University, Busan, Republic of Korea
    Cancer Lett 271:25-33. 2008
    ..Taken together, these results suggest that anti-cancer activities induced by PTX-2 may be mediated in part through suppression of constitutive NF-kappaB activity...
  88. doi Induction of G2/M arrest, endoreduplication, and apoptosis by actin depolymerization agent pextenotoxin-2 in human leukemia cells, involving activation of ERK and JNK
    Dong Oh Moon
    Faculty of Applied Marine Science, Cheju National University, Jeju Special Self Governing Province 690 756, South Korea
    Biochem Pharmacol 76:312-21. 2008
    ..These molecular mechanisms provide that PTX-2 induces G2/M phase arrest, endoreduplication, and apoptosis through the ERK and JNK signal pathway via actin depolymerization...
  89. doi Simple chemical transformation of lignocellulosic biomass into furans for fuels and chemicals
    Joseph B Binder
    Department of Chemistry, University of Wisconsin Madison, Madison, Wisconsin 53706, USA
    J Am Chem Soc 131:1979-85. 2009
    ....
  90. ncbi Free flowing solid dispersions of the anti-HIV drug UC 781 with Poloxamer 407 and a maximum amount of TPGS 1000: investigating the relationship between physicochemical characteristics and dissolution behaviour
    Caroline Goddeeris
    Laboratory of Pharmacotechnology and Biopharmacy, Catholic University of Leuven, Herestraat 49, B 3000 Leuven, Belgium
    Eur J Pharm Sci 35:104-13. 2008
    ..Formulation of solid dispersions did however not further improve the drug dissolution rate compared to that of physical mixtures. Nonetheless, variability of dissolution results was considerably reduced upon solid dispersion formulation...
  91. ncbi Characterization of F-actin depolymerization as a major toxic event induced by pectenotoxin-6 in neuroblastoma cells
    Francisco Leira
    ANFACO CECOPESCA, Campus Universitario de Vigo, 36310, Vigo, Spain
    Biochem Pharmacol 63:1979-88. 2002
    ..Therefore, we conclude that cytoskeletal disruption is a key mechanism of PTX6-induced toxicity in eukaryotic cells...
  92. doi Arctigenin blocks the unfolded protein response and shows therapeutic antitumor activity
    Ju Young Kim
    Department of Food Science and Biotechnology, Kyungnam University, Masan, Korea
    J Cell Physiol 224:33-40. 2010
    ..Furthermore, ARC-G suppressed tumor growth of colon cancer HT-29 xenografts. Our results demonstrate that ARC-G can be served as a novel type of antitumor agent targeting the UPR in glucose-deprived solid tumors...
  93. ncbi New cytotoxic monotetrahydrofuran annonaceous acetogenins from Annona muricata
    Chih Chuang Liaw
    Graduate Institute of Natural Products, Kaohsiung Medical University, Kaohsiung 807, Taiwan, Republic of China
    J Nat Prod 65:470-5. 2002
    ..These new acetogenins exhibited significant activity in in vitro cytotoxic assays against two human hepatoma cell lines, Hep G(2) and 2,2,15. Compound 5 showed a high selectivity toward the Hep 2,2,15 cell line...
  94. ncbi Annonacin, a mono-tetrahydrofuran acetogenin, arrests cancer cells at the G1 phase and causes cytotoxicity in a Bax- and caspase-3-related pathway
    Shyng Shiou F Yuan
    Department of Obstetrics and Gynecology, Kaohsiung Medical University, Kaohsiung, Taiwan 807, ROC
    Life Sci 72:2853-61. 2003
    ..It also induced Bax expression, enhanced caspase-3 activity, and caused apoptotic cell death in T24 cells. In summary, these results suggest that annonacin is potentially a promising anti-cancer compound...
  95. doi Arctigenin, a phenylpropanoid dibenzylbutyrolactone lignan, inhibits type I-IV allergic inflammation and pro-inflammatory enzymes
    Ji Yun Lee
    Division of Pathophysiology and Pharmacology, College of Pharmacy, Chung Ang University, Seoul, Korea
    Arch Pharm Res 33:947-57. 2010
    ..Our results show that arctigenin significantly inhibited B- and T-cell mediated allergic inflammation as well as pro-inflammatory enzymes...
  96. ncbi Arctigenin protects cultured cortical neurons from glutamate-induced neurodegeneration by binding to kainate receptor
    Young P Jang
    College of Pharmacy, Seoul National University, San 56 1, Shillim Dong, Kwanak gu, Seoul 151 742, Korea
    J Neurosci Res 68:233-40. 2002
    ..These results suggest that arctigenin exerted significant neuroprotective effects on glutamate-injured primary cultures of rat cortical cells by directly binding to kainic acid receptors and partly scavenging of free radicals...
  97. ncbi Sirtuin 2 inhibitors rescue alpha-synuclein-mediated toxicity in models of Parkinson's disease
    Tiago Fleming Outeiro
    Alzheimer s Research Unit, MGH, Harvard Medical School, CNY 114, 16th Street, Charlestown, MA 02129, USA
    Science 317:516-9. 2007
    ..Furthermore, the inhibitors protected against dopaminergic cell death both in vitro and in a Drosophila model of Parkinson's disease. The results suggest a link between neurodegeneration and aging...
  98. pmc A comprehensive comparison of DNA replication past 2-deoxyribose and its tetrahydrofuran analog in Escherichia coli
    Kelly M Kroeger
    Department of Chemistry, Johns Hopkins University, 3400 N Charles Street, Baltimore, MD 21218, USA
    Nucleic Acids Res 32:5480-5. 2004
    ..Our studies reveal that in uninduced E.coli the effects of individual polymerases in the replication of plasmids containing F or AP are distinct. However, when cells are SOS-induced, the biological effects of F and AP are similar...
  99. ncbi Annonaceous acetogenins: the hydroxyl groups and THF rings are crucial structural elements for targeting the mitochondria, demonstration with the synthesis of fluorescent squamocin analogues
    Séverine Derbré
    Laboratoire de Pharmacognosie associé au CNRS, UMR 8076, Centre d Etudes Pharmaceutiques, Universite Paris Sud 11, 5, rue Jean Baptiste Clement, 92296 Chatenay Malabry Cedex, France
    Chembiochem 6:979-82. 2005
  100. ncbi Probing the configurations of formamidopyrimidine lesions Fapy.dA and Fapy.dG in DNA using endonuclease IV
    Jennifer N Patro
    Department of Chemistry, Johns Hopkins University, 3400 North Charles Street, Baltimore, Maryland 21218, USA
    Biochemistry 43:13397-403. 2004
    ..Endo IV incises Fapy.dG to less than 5% under comparable reaction conditions, suggesting that the lesion exists almost exclusively as its beta-anomer in DNA...
  101. ncbi Bilobalide and neuroprotection
    Francis V DeFeudis
    Institute for BioScience, 153 West Main Street, Westboro, MA 01581, USA
    Pharmacol Res 46:565-8. 2002
    ..As multiple modes of action may apply to bilobalide, it could be useful in developing therapy for disorders involving cerebral ischemia and neurodegeneration...

Research Grants76

  1. NITROGEN CONTAINING NATURAL PRODUCTS
    Stephen Martin; Fiscal Year: 2001
    ..involve inter- and intramolecular reactions of iminium salts with nucleophilic partners, especially oxygenated furans; and (4) explore 1,2-metallate rearrangements as a novel entry to unsaturated nitrogen compounds...
  2. Synthesis of Medicinally Important Heterocycles
    RICHARD LAROCK; Fiscal Year: 2007
    ..benzolactams, dihydropyrimidines, 2-furanones, 2-pyrrolinones, benzopyrans, chromones and heteroatom analogues, furans, thiophenes, pyrroles, oxazoles, isoxazoles, pyrazoles, pyridines, quinolines, coumarins, indenes, indenones, ..
  3. Heterocyclic /Carbocyclic Libraries for High Throughput
    RICHARD LAROCK; Fiscal Year: 2006
    ..chromones, benzothiophenes, benzoselenophenes, phthalides, isocoumarins, isochromenes, isoquinolines, quinolines, furans, isoxazoles and various spirotrienones...
  4. Pilot-Scale Heterocyclic and Carbocyclic Libraries for High Throughout Screening
    RICHARD LAROCK; Fiscal Year: 2007
    ..chromones, benzothiophenes, benzoselenophenes, phthalides, isocoumarins, isochromenes, isoquinolines, quinolines, furans, isoxazoles and various spirotrienones...
  5. Pilot-Scale Heterocyclic and Carbocyclic Libraries for High Throughout Screening
    RICHARD LAROCK; Fiscal Year: 2009
    ..chromones, benzothiophenes, benzoselenophenes, phthalides, isocoumarins, isochromenes, isoquinolines, quinolines, furans, isoxazoles and various spirotrienones...
  6. Synthesis of Medicinally Important Heterocycles
    RICHARD LAROCK; Fiscal Year: 2005
    ..benzolactams, dihydropyrimidines, 2-furanones, 2-pyrrolinones, benzopyrans, chromones and heteroatom analogues, furans, thiophenes, pyrroles, oxazoles, isoxazoles, pyrazoles, pyridines, quinolines, coumarins, indenes, indenones, ..
  7. Synthesis of Medicinally Important Heterocycles
    RICHARD LAROCK; Fiscal Year: 2004
    ..benzolactams, dihydropyrimidines, 2-furanones, 2-pyrrolinones, benzopyrans, chromones and heteroatom analogues, furans, thiophenes, pyrroles, oxazoles, isoxazoles, pyrazoles, pyridines, quinolines, coumarins, indenes, indenones, ..
  8. Synthesis of Medicinally Important Heterocycles
    RICHARD LAROCK; Fiscal Year: 2006
    ..benzolactams, dihydropyrimidines, 2-furanones, 2-pyrrolinones, benzopyrans, chromones and heteroatom analogues, furans, thiophenes, pyrroles, oxazoles, isoxazoles, pyrazoles, pyridines, quinolines, coumarins, indenes, indenones, ..
  9. Estimating Dioxin Exposure from Indoor Woodsmoke and the Burning of Plastics
    Kirk R Smith; Fiscal Year: 2010
    ..Dioxins and furans, some of the most toxic substances in the world, are formed in wood combustion along with the other hundreds of ..
  10. SYNTHESIS OF NITROGEN-CONTAINING NATURAL PRODUCTS
    Stephen Martin; Fiscal Year: 1993
    ..and intramolecular reactions of iminium salts with electron-rich nucleophilic partners, especially oxygenated furans. In the arena of total synthesis, we will: (1) continue development of intramolecular hetero Diels-Alder reactions ..
  11. SYNTHESIS OF NITROGEN-CONTAINING NATURAL PRODUCTS
    Stephen Martin; Fiscal Year: 1992
    ..and intramolecular reactions of iminium salts with electron-rich nucleophilic partners, especially oxygenated furans. In the arena of total synthesis, we will: (1) continue development of intramolecular hetero Diels-Alder reactions ..
  12. NITROGEN CONTAINING NATURAL PRODUCTS
    Stephen Martin; Fiscal Year: 2000
    ..involve inter- and intramolecular reactions of iminium salts with nucleophilic partners, especially oxygenated furans; and (4) explore 1,2-metallate rearrangements as a novel entry to unsaturated nitrogen compounds...
  13. NITROGEN CONTAINING NATURAL PRODUCTS
    Stephen Martin; Fiscal Year: 1999
    ..involve inter- and intramolecular reactions of iminium salts with nucleophilic partners, especially oxygenated furans; and (4) explore 1,2-metallate rearrangements as a novel entry to unsaturated nitrogen compounds...
  14. EARLY TRANSITION METAL CATALYSTS FOR ORGANIC SYNTHESIS
    STEPHEN BUCHWALD; Fiscal Year: 1992
    ..reductions of ketones to silyl ethers; 9) The conversion of oxindoles to indoles and butenolides to furans; 10) The conversion of carboxylic acids to alcohols and to aldehydes; and 11) The conversion of nitriles into ..
  15. Effects of Dioxin on Vietnamese Civilians
    David Carpenter; Fiscal Year: 2004
    ..Blood will be obtained from the mother for serum dioxin and furans (total plus 17 individual isomers plus WHO TEQs including PCBs, performed by AXYS Analytical Services Ltd...
  16. Novel Direct Approaches Toward Bioactive Heterocycles
    Vladimir Gevorgyan; Fiscal Year: 2010
    ..is devoted to the investigation and development of novel cycloisomerization approaches toward monocyclic and fused furans, pyrroles, and thiophenes, and to the development of cascade migration/cyclization methodologies en route to ..
  17. Tetrahydrofurans, Tetrahydropyrans and 2H-Furanones
    CHRISTOPHER SPILLING; Fiscal Year: 2006
    ..Tetrahydro furans and pyrans are common structural features in a number of important classes of natural product...
  18. Tetrahydrofurans, Tetrahydropyrans and 2H-Furanones
    CHRISTOPHER SPILLING; Fiscal Year: 2007
    ..Tetrahydro furans and pyrans are common structural features in a number of important classes of natural product...
  19. Tetrahydrofurans, Tetrahydropyrans and 2H-Furanones
    CHRISTOPHER SPILLING; Fiscal Year: 2009
    ..Tetrahydro furans and pyrans are common structural features in a number of important classes of natural product...
  20. New Technologies for the Remediation
    Eric Betterton; Fiscal Year: 2005
    ..high-temperature incineration of the carbon may produce much more toxic contaminants such as dioxins and furans whose release to the atmosphere might pose an even greater health risk...
  21. NATURALLY OCCURRING FOOD TOXICANTS
    Benjamin Wilson; Fiscal Year: 1980
    ..The principal toxins to be studied are lung- and liver-toxic, 3-substituted furans which include stress metabolites of the sweet potato, Ipomoea batatas: normal metabolites of the purple mint plant,..
  22. DEVELOPING AN UNDERSTANDING OF ASYMMETRIC INDUCTION
    Patrick Walsh; Fiscal Year: 2009
    ..be applied to the synthesis of enantiomerically enriched heterocycles bearing important pharmacophores, such as furans and pyridines. We have also developed several new routes to pyranones, furanosidic aldehydes, furans, and pyrroles...
  23. DEVELOPING AN UNDERSTANDING OF ASYMMETRIC INDUCTION
    Patrick J Walsh; Fiscal Year: 2010
    ..be applied to the synthesis of enantiomerically enriched heterocycles bearing important pharmacophores, such as furans and pyridines. We have also developed several new routes to pyranones, furanosidic aldehydes, furans, and pyrroles...
  24. DEVELOPING AN UNDERSTANDING OF ASYMMETRIC INDUCTION
    Patrick Walsh; Fiscal Year: 2007
    ..be applied to the synthesis of enantiomerically enriched heterocycles bearing important pharmacophores, such as furans and pyridines. We have also developed several new routes to pyranones, furanosidic aldehydes, furans, and pyrroles...
  25. DEVELOPING AN UNDERSTANDING OF ASYMMETRIC INDUCTION
    Patrick J Walsh; Fiscal Year: 2010
    ..be applied to the synthesis of enantiomerically enriched heterocycles bearing important pharmacophores, such as furans and pyridines. We have also developed several new routes to pyranones, furanosidic aldehydes, furans, and pyrroles...
  26. CONSEQUENCES OF AhR-MEDIATED SIGNALING IN DENDRITIC CELLS
    David Shepherd; Fiscal Year: 2002
    ..Many of these chemicals that include the dioxins, furans, and polychlorinated biphenyls (PCBs) persist for very long periods of time in the environment and have the ..
  27. Strategies for the Syntheses of Bioactive Targets
    Stephen Martin; Fiscal Year: 2003
    ..A, vineomycinone B 2, kidamycin and rubiflavin A feature intramolecular [4+2] cycloadditions of sugar-substituted furans with benzynes to give oxabicycloheptadienes that undergo acid-catalyzed rearrangements to furnish C-glycosylated ..
  28. Strategies for the Syntheses of Bioactive Targets
    Stephen Martin; Fiscal Year: 2005
    ..A, vineomycinone B 2, kidamycin and rubiflavin A feature intramolecular [4+2] cycloadditions of sugar-substituted furans with benzynes to give oxabicycloheptadienes that undergo acid-catalyzed rearrangements to furnish C-glycosylated ..
  29. Strategies for the Syntheses of Bioactive Targets
    Stephen Martin; Fiscal Year: 2006
    ..A, vineomycinone B 2, kidamycin and rubiflavin A feature intramolecular [4+2] cycloadditions of sugar-substituted furans with benzynes to give oxabicycloheptadienes that undergo acid-catalyzed rearrangements to furnish C-glycosylated ..
  30. Strategies for the Syntheses of Bioactive Targets
    Stephen Martin; Fiscal Year: 2004
    ..A, vineomycinone B 2, kidamycin and rubiflavin A feature intramolecular [4+2] cycloadditions of sugar-substituted furans with benzynes to give oxabicycloheptadienes that undergo acid-catalyzed rearrangements to furnish C-glycosylated ..
  31. Strategies for the Syntheses of Bioactive Targets
    Stephen Martin; Fiscal Year: 2006
    ..A, vineomycinone B 2, kidamycin and rubiflavin A feature intramolecular [4+2] cycloadditions of sugar-substituted furans with benzynes to give oxabicycloheptadienes that undergo acid-catalyzed rearrangements to furnish C-glycosylated ..
  32. Novel Direct Approaches Toward Bioactive Heterocycles
    Vladimir Gevorgyan; Fiscal Year: 2009
    ..is devoted to the investigation and development of novel cycloisomerization approaches toward monocyclic and fused furans, pyrroles, and thiophenes, and to the development of cascade migration/cyclization methodologies en route to ..
  33. Novel Direct Approaches Toward Bioactive Heterocycles
    Vladimir Gevorgyan; Fiscal Year: 2007
    ..is devoted to the investigation and development of novel cycloisomerization approaches toward monocyclic and fused furans, pyrroles, and thiophenes, and to the development of cascade migration/cyclization methodologies en route to ..
  34. Novel Direct Approaches Toward Bioactive Heterocycles
    Vladimir Gevorgyan; Fiscal Year: 2006
    ..is devoted to the investigation and development of novel cycloisomerization approaches toward monocyclic and fused furans, pyrroles, and thiophenes, and to the development of cascade migration/cyclization methodologies en route to ..
  35. HETEROCYCLIC RING COMPOUNDS FOR ALKALOID SYNTHESIS
    Albert Padwa; Fiscal Year: 2006
    ..Among the reactions to be studied are [4+2]-cycloaddition reactions of amido and thio-substituted furans and other heteroaromatics as a method for preparing novel azapolycyclic rings...
  36. HETEROCYCLIC RING COMPOUNDS FOR ALKALOID SYNTHESIS
    Albert Padwa; Fiscal Year: 2005
    ..Among the reactions to be studied are [4+2]-cycloaddition reactions of amido and thio-substituted furans and other heteroaromatics as a method for preparing novel azapolycyclic rings...
  37. HETEROCYCLIC RING COMPOUNDS FOR ALKALOID SYNTHESIS
    Albert Padwa; Fiscal Year: 2005
    ..Among the reactions to be studied are [4+2]-cycloaddition reactions of amido and thio-substituted furans and other heteroaromatics as a method for preparing novel azapolycyclic rings...
  38. HETEROCYCLIC RING COMPOUNDS FOR ALKALOID SYNTHESIS
    Albert Padwa; Fiscal Year: 2004
    ..Among the reactions to be studied are [4+2]-cycloaddition reactions of amido and thio-substituted furans and other heteroaromatics as a method for preparing novel azapolycyclic rings...
  39. HETEROCYCLIC RING COMPOUNDS FOR ALKALOID SYNTHESIS
    Albert Padwa; Fiscal Year: 2007
    ..Among the reactions to be studied are [4+2]-cycloaddition reactions of amido and thio-substituted furans and other heteroaromatics as a method for preparing novel azapolycyclic rings...
  40. STRUCTURE-TOXICITY RELATIONSHIPS AMONG HETEROCYCLES
    John Garst; Fiscal Year: 1980
    ..of PK lacking the structural features producing pulmonary effects and many natural, synthetic, and commerical furans retain high toxicity. They are, however, much less potent and lung selective than PK...
  41. FURAN LUNG TOXINS: ORGAN SPECIFICITY AND METABOLISM
    ROBERT WILEY; Fiscal Year: 1980
    Several simple heterocyclic compounds, such as furans and thiophenes, are known to damage mammalian lung, liver, and kidney. Some of these compounds occur naturally, primarily as smog components, in cotton mill dust, and in certain plants...
  42. STRATEGIES FOR THE SYNTHESIS OF BIOACTIVE TARGETS
    Stephen Martin; Fiscal Year: 1999
    ..basic strategies for the syntheses of these compounds are unique and involve the stereoselective elaboration of furans and hydropyrans derived therefrom, asymmetric cyclopropanations, ring closing metatheses, and vinylogous aldol ..
  43. STRATEGIES FOR THE SYNTHESIS OF BIOACTIVE TARGETS
    Stephen Martin; Fiscal Year: 2000
    ..basic strategies for the syntheses of these compounds are unique and involve the stereoselective elaboration of furans and hydropyrans derived therefrom, asymmetric cyclopropanations, ring closing metatheses, and vinylogous aldol ..
  44. STRATEGIES FOR THE SYNTHESIS OF BIOACTIVE TARGETS
    Stephen Martin; Fiscal Year: 2001
    ..basic strategies for the syntheses of these compounds are unique and involve the stereoselective elaboration of furans and hydropyrans derived therefrom, asymmetric cyclopropanations, ring closing metatheses, and vinylogous aldol ..
  45. STRATEGIES FOR THE SYNTHESIS OF BIOACTIVE TARGETS
    Stephen Martin; Fiscal Year: 2002
    ..basic strategies for the syntheses of these compounds are unique and involve the stereoselective elaboration of furans and hydropyrans derived therefrom, asymmetric cyclopropanations, ring closing metatheses, and vinylogous aldol ..
  46. HYBRID TANDEM MASS SPECTROMETRY OF PEPTIDE CONJUGATES
    Simon Gaskell; Fiscal Year: 1992
    ..will be applied to the analysis of glutathione conjugates (formed in vivo and in vitro) of several substituted furans, a class of compounds which shows marked toxicological variability with respect to the protective effect of ..
  47. HETEROCYCLE-METAL PI-COMPLEXES IN ORGANIC SYNTHESIS
    LANNY LIEBESKIND; Fiscal Year: 1992
    ..for the regio- and stereospecific synthesis of highly substituted heterocycles (dihydro- and tetrahydro- pyrans, furans, piperidines and pyrroles) is proposed...
  48. HETEROCYCLE-METAL PI-COMPLEXES IN ORGANIC SYNTHESIS
    LANNY LIEBESKIND; Fiscal Year: 1991
    ..for the regio- and stereospecific synthesis of highly substituted heterocycles (dihydro- and tetrahydro- pyrans, furans, piperidines and pyrroles) is proposed...
  49. HETEROCYCLE-METAL PI-COMPLEXES IN ORGANIC SYNTHESIS
    LANNY LIEBESKIND; Fiscal Year: 1990
    ..for the regio- and stereospecific synthesis of highly substituted heterocycles (dihydro- and tetrahydro- pyrans, furans, piperidines and pyrroles) is proposed...
  50. NEW TEST METHOD FOR DIOXINS IN HUMANS AND ANIMALS
    Randy Allen; Fiscal Year: 2000
    Dioxins and furans comprise one of the most deadly and feared families of pollutants in the world...
  51. NOVEL APPROACHES TO ALKALOID SYNTHESIS
    Patrick Mariano; Fiscal Year: 2003
    ..by applications to stereocontrolled preparation of polyhydroxylated-piperidines and tetrahydro-pyrans and -furans. In future studies, the preparative potential of oxidative methods for oxonium cation generation will be probed ..
  52. STRATEGIES FOR THE SYNTHESIS OF BIOACTIVE TARGETS
    Stephen Martin; Fiscal Year: 1991
    ..of the dipolar cycloadditions of nitrile oxides will be developed, and extensions of our strategy exploiting furans and hydropyrans as key intermediates for the asymmetric syntheses of natural products and selected skeletal ..
  53. Active Site Models of CYP4 Enzymes
    Allan Rettie; Fiscal Year: 2009
    ..with the bioactivation of a diverse array of pro-toxins including carcinogenic aromatic amines and pneumotoxic furans, while also maintaining to-hydroxylase selectivity for fatty acids and alkyl hydrocarbons...
  54. STRATEGIES FOR THE SYNTHESIS OF BIOACTIVE TARGETS
    Stephen Martin; Fiscal Year: 1992
    ..of the dipolar cycloadditions of nitrile oxides will be developed, and extensions of our strategy exploiting furans and hydropyrans as key intermediates for the asymmetric syntheses of natural products and selected skeletal ..
  55. NOVEL APPROACHES TO ALKALOID SYNTHESIS
    Patrick Mariano; Fiscal Year: 2004
    ..by applications to stereocontrolled preparation of polyhydroxylated-piperidines and tetrahydro-pyrans and -furans. In future studies, the preparative potential of oxidative methods for oxonium cation generation will be probed ..
  56. Active Site Models of CYP4 Enzymes
    Allan Rettie; Fiscal Year: 2007
    ..with the bioactivation of a diverse array of pro-toxins including carcinogenic aromatic amines and pneumotoxic furans, while also maintaining to-hydroxylase selectivity for fatty acids and alkyl hydrocarbons...
  57. NOVEL APPROACHES TO ALKALOID SYNTHESIS
    Patrick Mariano; Fiscal Year: 2001
    ..by applications to stereocontrolled preparation of polyhydroxylated-piperidines and tetrahydro-pyrans and -furans. In future studies, the preparative potential of oxidative methods for oxonium cation generation will be probed ..
  58. STRATEGIES FOR THE SYNTHESIS OF BIOACTIVE TARGETS
    Stephen Martin; Fiscal Year: 1993
    ..of the dipolar cycloadditions of nitrile oxides will be developed, and extensions of our strategy exploiting furans and hydropyrans as key intermediates for the asymmetric syntheses of natural products and selected skeletal ..
  59. Active Site Models of CYP4 Enzymes
    ALLAN EDWARD RETTIE; Fiscal Year: 2010
    ..with the bioactivation of a diverse array of pro-toxins including carcinogenic aromatic amines and pneumotoxic furans, while also maintaining to-hydroxylase selectivity for fatty acids and alkyl hydrocarbons...
  60. NOVEL APPROACHES TO ALKALOID SYNTHESIS
    Patrick Mariano; Fiscal Year: 2002
    ..by applications to stereocontrolled preparation of polyhydroxylated-piperidines and tetrahydro-pyrans and -furans. In future studies, the preparative potential of oxidative methods for oxonium cation generation will be probed ..
  61. Total Synthesis of Polygaloides A & B
    ERICK IEZZI; Fiscal Year: 2005
    ..products, which will be accomplished by utilizing [4 + 3] cycloaddition reactions between 2,3-disubstituted furans and vinyl oxocarbenium ions to generate, in a single step, a complex segment of the molecules' unprecedented fused ..
  62. Total Synthesis of Polygaloides A & B
    ERICK IEZZI; Fiscal Year: 2004
    ..products, which will be accomplished by utilizing [4 + 3] cycloaddition reactions between 2,3-disubstituted furans and vinyl oxocarbenium ions to generate, in a single step, a complex segment of the molecules' unprecedented fused ..
  63. Use of 2-Amido Substituted Furans for Alkaloid Synthesis
    Mickea Rose; Fiscal Year: 2003
    ..The project involves novel methods towards the synthesis of 2-amido furans from pyrrolidinone intermediates. Cyclic amides are widely regarded as useful precursors for N-acyliminium ions...
  64. Use of 2-Amido Substituted Furans for Alkaloid Synthesis
    Mickea Rose; Fiscal Year: 2005
    ..The project involves novel methods towards the synthesis of 2-amido furans from pyrrolidinone intermediates. Cyclic amides are widely regarded as useful precursors for N-acyliminium ions...
  65. DEVELOPMENT OF AH RECEPTOR-BASED TEQ TEST
    JOHN WILLEY; Fiscal Year: 2000
    ..The resulting system would be used to quantify AhR-binding toxicants such as dioxins, furans, and PCBs from clinical samples such as blood, serum or tissue, food samples such as meat fat, or environmental ..
  66. Use of 2-Amido Substituted Furans for Alkaloid Synthesis
    Mickea Rose; Fiscal Year: 2006
    ..The project involves novel methods towards the synthesis of 2-amido furans from pyrrolidinone intermediates. Cyclic amides are widely regarded as useful precursors for N-acyliminium ions...
  67. Use of 2-Amido Substituted Furans for Alkaloid Synthesis
    Mickea Rose; Fiscal Year: 2004
    ..The project involves novel methods towards the synthesis of 2-amido furans from pyrrolidinone intermediates. Cyclic amides are widely regarded as useful precursors for N-acyliminium ions...
  68. HETEROCYCLE-METAL PI COMPLEXES IN ORGANIC SYNTHESIS
    LANNY LIEBESKIND; Fiscal Year: 1993
    ..for the regio- and enantiospecific synthesis of highly substituted heterocycles (dihydro- and tetrahydropyrans, furans, piperidines and pyrroles) is described...
  69. Synthesis of Bioactive Marine Natural Products
    Emmanuel A Theodorakis; Fiscal Year: 2010
    ..The proposed methods stem from the unexplored reactivity of electronically rich species, such as dienes and furans, during cycloaddition reactions and highlight the potential of these reactions for the construction of highly ..
  70. SWEET POTATO TOXINS
    Leo Burka; Fiscal Year: 1980
    ..The research outlined in the proposal is concerned with the metabolic activation of one of the lung toxic furans, 4-ipomeanol, in animals and the biosynthesis of furanosesquiterpenes in the plant...
  71. Synthesis of Bioactive Marine Natural Products
    Emmanuel Theodorakis; Fiscal Year: 2009
    ..The proposed methods stem from the unexplored reactivity of electronically rich species, such as dienes and furans, during cycloaddition reactions and highlight the potential of these reactions for the construction of highly ..
  72. Development of Spirodiepoxide-Based Methods of Chemical Synthesis
    Lawrence Williams; Fiscal Year: 2009
    ..SDE formation and intramolecular heteroatom nucleophile SDE-openings focused on the synthesis of pyrans and furans and will be utilized in the synthesis of psymberin and pectenotoxin 4, which are antitumor agents...
  73. Development of Spirodiepoxide-Based Methods of Chemical Synthesis
    Lawrence Williams; Fiscal Year: 2007
    ..SDE formation and intramolecular heteroatom nucleophile SDE-openings focused on the synthesis of pyrans and furans and will be utilized in the synthesis of psymberin and pectenotoxin 4, which are antitumor agents...