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 Eribulin monotherapy versus treatment of physician's choice in patients with metastatic breast cancer (EMBRACE): a phase 3 open-label randomised study
    Javier Cortes
    Vall d Hebron University Hospital, Vall d Hebron Institute of Oncology, Barcelona, Spain
    Lancet 377:914-23. 2011
  4. pmc Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941
    Florence I Raynaud
    Cancer Research UK Centre for Cancer Therapeutics, The Institute of Cancer Research, Sutton, Surrey, UK
    Mol Cancer Ther 8:1725-38. 2009
  5. 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
  6. 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
  7. ncbi 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
  8. ncbi 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
  9. 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
  10. pmc Eribulin binds at microtubule ends to a single site on tubulin to suppress dynamic instability
    Jennifer A Smith
    Department of Molecular, Cellular, and Developmental Biology and Neuroscience Research Institute, University of California, Santa Barbara, California 93106, USA
    Biochemistry 49:1331-7. 2010

Detail Information

Publications387 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 Eribulin monotherapy versus treatment of physician's choice in patients with metastatic breast cancer (EMBRACE): a phase 3 open-label randomised study
    Javier Cortes
    Vall d Hebron University Hospital, Vall d Hebron Institute of Oncology, Barcelona, Spain
    Lancet 377:914-23. 2011
    ..Eribulin mesilate is a non-taxane microtubule dynamics inhibitor with a novel mode of action. We aimed to compare overall survival of heavily pretreated patients receiving eribulin versus currently available treatments...
  4. pmc Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941
    Florence I Raynaud
    Cancer Research UK Centre for Cancer Therapeutics, The Institute of Cancer Research, Sutton, Surrey, UK
    Mol Cancer Ther 8:1725-38. 2009
    ..Together, these data support the development of GDC-0941 as a potent, orally bioavailable inhibitor of phosphatidylinositide 3-kinase. GDC-0941 has recently entered phase I clinical trials...
  5. 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...
  6. 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...
  7. ncbi 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...
  8. ncbi 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...
  9. 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...
  10. pmc Eribulin binds at microtubule ends to a single site on tubulin to suppress dynamic instability
    Jennifer A Smith
    Department of Molecular, Cellular, and Developmental Biology and Neuroscience Research Institute, University of California, Santa Barbara, California 93106, USA
    Biochemistry 49:1331-7. 2010
    ..Overall, our results indicate that eribulin binds with high affinity to microtubule plus ends and thereby suppresses dynamic instability...
  11. 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
    ....
  12. pmc DNA repair of clustered lesions in mammalian cells: involvement of non-homologous end-joining
    Svitlana Malyarchuk
    Department of Molecular and Cellular Physiology, Louisiana Health Sciences Center, Shreveport, LA 71130, USA
    Nucleic Acids Res 36:4872-82. 2008
    ..NHEJ), we hypothesized that NHEJ would repair DSBs formed during the removal of clustered tetrahydrofurans (furans)...
  13. 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...
  14. ncbi Arctigenin preferentially induces tumor cell death under glucose deprivation by inhibiting cellular energy metabolism
    Yuan Gu
    Department of Tumor Pharmacology, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China
    Biochem Pharmacol 84:468-76. 2012
    ..Hence, we propose that the combination of arctigenin and 2DG may represent a promising new cancer therapy with minimal normal tissue toxicity...
  15. 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
    ....
  16. 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...
  17. 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...
  18. 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
    ....
  19. 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...
  20. 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...
  21. 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...
  22. 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...
  23. 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
    ....
  24. ncbi 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...
  25. 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...
  26. 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...
  27. 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
    ....
  28. ncbi Phase II study of eribulin mesylate, a halichondrin B analog, in patients with metastatic breast cancer previously treated with an anthracycline and a taxane
    Linda T Vahdat
    Weill Medical College of Cornell University, Division of Hematology Oncology, New York, NY 10021, USA
    J Clin Oncol 27:2954-61. 2009
    ..This open-label, single-arm, phase II study evaluated efficacy and tolerability of eribulin in heavily pretreated patients with metastatic breast cancer (MBC)...
  29. pmc Brominated furanones inhibit biofilm formation by Salmonella enterica serovar Typhimurium
    Joost C A Janssens
    Centre of Microbial and Plant Genetics, Katholieke Universiteit Leuven, Leuven, Belgium
    Appl Environ Microbiol 74:6639-48. 2008
    ..Conclusively, this work demonstrates that particular brominated furanones have potential in the prevention of biofilm formation by Salmonella serovar Typhimurium...
  30. ncbi 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...
  31. ncbi Phase II study of the halichondrin B analog eribulin mesylate in patients with locally advanced or metastatic breast cancer previously treated with an anthracycline, a taxane, and capecitabine
    Javier Cortes
    Vall d Hebron University Hospital, Barcelona, Spain
    J Clin Oncol 28:3922-8. 2010
    ....
  32. ncbi Xanthatin and xanthinosin from the burs of Xanthium strumarium L. as potential anticancer agents
    Irving Ramirez-Erosa
    Department of Plant Sciences, University of Saskatchewan, Saskatoon, SK S7N 5A8, Canada
    Can J Physiol Pharmacol 85:1160-72. 2007
    ..strumarium yielded xanthatin and xanthinosin in high yields. This is the first time that these compounds have been reported in the burs of X. strumarium. Their IC50 values are also reported herein...
  33. ncbi Biological activities of xanthatin from Xanthium strumarium leaves
    Endalkachew Nibret
    Institut für Pharmazie und molekulare Biotechnologie, Universitat Heidelberg, Im Neuenheimer Feld 364, 69120, Heidelberg, Germany
    Phytother Res 25:1883-90. 2011
    ....
  34. ncbi Arctigenin suppresses unfolded protein response and sensitizes glucose deprivation-mediated cytotoxicity of cancer cells
    Shengrong Sun
    Department of Breast and Thyroid Surgery, Wuhan University Renmin Hospital, Wuhan, China
    Planta Med 77:141-5. 2011
    ..These observations bring a new insight into the mechanism of action of arctigenin and may lead to the design of new anticancer therapeutics...
  35. ncbi Advances in therapy: eribulin improves survival for metastatic breast cancer
    Patrick G Morris
    Breast Cancer Medicine Service, Memorial Sloan Kettering Cancer Center, Evelyn H Lauder Breast Center, New York, USA
    Anticancer Drugs 21:885-9. 2010
    ..Future studies will investigate the potential role of eribulin in other settings, including for early breast cancer, to ascertain how to optimally incorporate this new agent into current treatment paradigms...
  36. ncbi Tetramic and tetronic acids: an update on new derivatives and biological aspects
    Rainer Schobert
    Organic Chemistry Laboratory, University of Bayreuth, Bayreuth, Germany
    Bioorg Med Chem 16:4203-21. 2008
    ..Important new members of the title compound families isolated since the year 2000 are covered as well as new biological aspects of some earlier congeners...
  37. 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...
  38. ncbi Eribulin induces irreversible mitotic blockade: implications of cell-based pharmacodynamics for in vivo efficacy under intermittent dosing conditions
    Murray J Towle
    Division of Biology, Eisai Inc, Andover, Massachusetts, USA
    Cancer Res 71:496-505. 2011
    ....
  39. ncbi Pectenotoxin-2 in single-cell isolates of Dinophysis caudata and Dinophysis acuta from the Galician Rías (NW Spain)
    M Luisa Fernández
    Centro Tecnológico del Mar, Fundación CETMAR, Eduardo Cabello s n, 36208 Vigo, Spain
    Toxicon 48:477-90. 2006
    ..Conclusive toxicological studies are required to elucidate the public health relevance of the different PTXs derivatives and to provide the scientific basis for regulations...
  40. ncbi Polychlorinated biphenyls, dioxins, and furans in weaned, free-ranging northern elephant seal pups from central California, USA
    Cathy Debier
    Unite de Biochimie de la Nutrition, Universite Catholique de Louvain, Croix du Sud 2 8, B 1348 Louvain la Neuve, Belgium
    Environ Toxicol Chem 24:629-33. 2005
    ..Our results suggest that NES pups, in contrast to pups of other pinnipeds in the eastern Pacific Ocean, are exposed to low levels of persistent organic pollutants, reflecting an open ocean signal...
  41. ncbi Comparison of neuropathy-inducing effects of eribulin mesylate, paclitaxel, and ixabepilone in mice
    Krystyna M Wozniak
    Johns Hopkins Brain Science Institute, Baltimore, Maryland 21205, USA
    Cancer Res 71:3952-62. 2011
    ..Overall, our findings indicate that eribulin mesylate induces less neuropathy in mice than paclitaxel or ixabepilone at equivalent MTD-based doses...
  42. ncbi Xanthatin induces G2/M cell cycle arrest and apoptosis in human gastric carcinoma MKN-45 cells
    Lei Zhang
    Department of Clinical Pharmacy, College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, Jiangsu, China
    Planta Med 78:890-5. 2012
    ..In conclusion, our results suggest that xanthatin may have therapeutic potential against human gastric carcinoma...
  43. 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 ..
  44. ncbi Comparison of electrokinetic properties of colloidal fullerenes (n-C60) formed using two procedures
    Jonathan Brant
    Department of Civil and Environmental Engineering, Rice University, Mail Stop 317, Houston, Texas 77251 1892, USA
    Environ Sci Technol 39:6343-51. 2005
    ....
  45. ncbi 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...
  46. ncbi PPARγ agonist from Chromolaena odorata
    Man Li Zhang
    School of Pharmaceutical Sciences, Hebei Medical University, 361 Zhongshan East Road, Shijiazhuang 050017, People s Republic of China
    J Nat Prod 75:2076-81. 2012
    ..All the compounds were evaluated for their PPARγ transactivation activity, and compound 6 showed moderate activity with an EC(50) value of 3.10 μM...
  47. ncbi A compound from smoke that promotes seed germination
    Gavin R Flematti
    School of Biomedical and Chemical Sciences, University of Western Australia, Crawley, WA 6009, Australia
    Science 305:977. 2004
    ..Here we show that 1 promotes germination of a number of plant species at a level similar to that observed with plant-derived smoke water...
  48. 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...
  49. ncbi 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...
  50. 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...
  51. 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...
  52. ncbi 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...
  53. ncbi 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...
  54. 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...
  55. 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...
  56. 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
    ....
  57. ncbi 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...
  58. 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...
  59. ncbi 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...
  60. ncbi 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...
  61. 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
    ....
  62. pmc Tautomycetin and tautomycin suppress the growth of medullary thyroid cancer cells via inhibition of glycogen synthase kinase-3beta
    Joel T Adler
    Endocrine Surgery Research Laboratories, Department of Surgery, University of Wisconsin, H4 750 Clinical Science Center, 600 Highland Avenue, Madison, WI 53792, USA
    Mol Cancer Ther 8:914-20. 2009
    ..Importantly, we describe a novel action of these compounds: inhibition of glycogen synthase kinase-3beta...
  63. ncbi 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...
  64. 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...
  65. 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...
  66. ncbi Daphnia magna mortality when exposed to titanium dioxide and fullerene (C60) nanoparticles
    Sarah B Lovern
    University of Wisconsin Milwaukee, Great Lakes WATER Institute, 600 E Greenfield Avenue, Milwaukee, Wisconsin 53204, USA
    Environ Toxicol Chem 25:1132-7. 2006
    ..Understanding the potential impacts of nanoparticles will help to identify the most appropriate nanotechnology to preserve the aquatic environment while advancing medical and environmental technology...
  67. ncbi 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...
  68. 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...
  69. 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...
  70. 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...
  71. 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...
  72. 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...
  73. 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
    ....
  74. 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...
  75. 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...
  76. ncbi 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...
  77. ncbi 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
    ....
  78. 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...
  79. 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...
  80. 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...
  81. ncbi Isoprostanes and isofurans as non-traditional risk factors for cardiovascular disease among Canadian Inuit
    Dalal Alkazemi
    School of Dietetics and Human Nutrition and Centre for Indigenous Peoples Nutrition and Environment, McGill University, Quebec, Canada
    Free Radic Res 46:1258-66. 2012
    ..We planned to examine the relationship between concentrations of plasma F₂-isoprostanes (F₂-IsoPs), isofurans (IsoFs), measures of obesity and various cardiometabolic risk factors...
  82. ncbi Relative differences in aryl hydrocarbon receptor-mediated response for 18 polybrominated and mixed halogenated dibenzo-p-dioxins and -furans in cell lines from four different species
    Helena Olsman
    Man Technology Environment Research Centre MTM, Department of Natural Science, University of Orebro, Orebro, Sweden
    Environ Toxicol Chem 26:2448-54. 2007
    ..there is a concern for persistent or increasing environmental levels of polybrominated dibenzo-p-dioxins/furans (PBDD/Fs) and mixed polychlorinated and polybrominated dibenzo-p-dioxins/furans (PXDD/Fs)...
  83. ncbi Identifying the important structural elements of brominated furanones for inhibiting biofilm formation by Escherichia coli
    Yongbin Han
    Department of Chemistry, Syracuse University, NY 13244, USA
    Bioorg Med Chem Lett 18:1006-10. 2008
    ..Furanones bearing monosubstituted bromide groups on saturated carbons were found to have a toxic effect that attenuates the bacterial growth...
  84. ncbi PI3K inhibitors prime neuroblastoma cells for chemotherapy by shifting the balance towards pro-apoptotic Bcl-2 proteins and enhanced mitochondrial apoptosis
    A Bender
    Department of Hematology Oncology, University Children s Hospital, Ulm, Germany
    Oncogene 30:494-503. 2011
    ..Thus, targeting PI3K presents a novel and promising strategy to sensitize neuroblastoma cells for chemotherapy-induced apoptosis, which has important implications for the development of targeted therapies for neuroblastoma...
  85. pmc Eribulin mesylate in patients with refractory cancers: a Phase I study
    Toru Mukohara
    Medical Oncology Hematology, Kobe University Hospital and Graduate School of Medicine, 7 5 1 Kusunoki cho, Chuo Ku, Kobe, 650 0017, Japan
    Invest New Drugs 30:1926-33. 2012
    ..4 mg/m(2) dose level. Eribulin mesylate, administered on Days 1 and 8 of a 21-day cycle, exhibits manageable tolerability at 1.4 mg/m(2). DLT was neutropenia...
  86. ncbi Meldrum's acid and related compounds in the synthesis of natural products and analogs
    Andrey S Ivanov
    Pharm Sintez, 117312, Vavilova Str 15, Moscow, Russia
    Chem Soc Rev 37:789-811. 2008
    ..This critical review focuses on applications of Meldrum's acid and its derivatives to the synthesis of natural products and analogs. It covers all relevant literature from 1991 to August 2007 (181 references)...
  87. pmc Hepatic clearance, but not gut availability, of erythromycin is altered in patients with end-stage renal disease
    H Sun
    Department of Biopharmaceutical Sciences, School of Pharmacy, University of California, San Francisco, San Francisco, California, USA
    Clin Pharmacol Ther 87:465-72. 2010
    ..As expected, plasma levels of CMPF and Indox were significantly higher in the patients than in the healthy controls. However, no correlation was observed between CL(H) of ER and the levels of uremic toxins...
  88. ncbi Effects of muscarinic antagonists on ZENK expression in the chicken retina
    Michaela Bitzer
    Section for Neurobiology of the Eye, University Eye Hospital, Calwerstr 7 1, 72076 Tuebingen, Germany
    Exp Eye Res 82:379-88. 2006
    ....
  89. ncbi Copper-catalyzed synthesis of substituted furans and pyrroles by heterocyclodehydration and tandem heterocyclodehydration-hydration of 3-yne-1,2-diols and 1-amino-3-yn-2-ol derivatives
    Bartolo Gabriele
    Dipartimento di Chimica e Tecnologie Chimiche, Universita della Calabria, Via P Bucci, 12 C, 87036 Arcavacata di Rende CS, Italy
    J Org Chem 78:4919-28. 2013
    ..heterocyclodehydration of readily available 3-yne-1,2-diols and 1-amino-3-yn-2-ol derivatives afforded substituted furans and pyrroles, respectively, in good to high yields (53-99%) under mild conditions (MeOH as the solvent, 80-100 °C,..
  90. ncbi Broad spectrum preclinical antitumor activity of eribulin (Halaven(R)): optimal effectiveness under intermittent dosing conditions
    Murray J Towle
    Discovery Biology, Oncology Product Creation Unit, Eisai Inc, Andover, MA, USA
    Anticancer Res 32:1611-9. 2012
    ..Here we extend those early studies by examining the effects of eribulin against a wider spectrum of human tumor xenografts in vivo, and by directly comparing the in vivo effectiveness of different dosing administration schedules...
  91. ncbi Association between dioxins/furans exposures and incinerator workers' hepatic function and blood lipids
    Suh Woan Hu
    Institute os Stomatology, Chung Shan Medical University, Taichung, Taiwan
    J Occup Environ Med 45:601-8. 2003
    This study examined the effects of dioxins/furans on blood lipids and hepatic function and assessed potential interaction between hepatitis B virus (HBV) infection and dioxins on hepatic function for 133 male workers of municipal waste ..
  92. ncbi Estimating sediment quality thresholds to prevent restrictions on fish consumption: Application to polychlorinated biphenyls and dioxins-furans in the Canadian Great Lakes
    Satyendra P Bhavsar
    Ontario Ministry of the Environment, Toronto, Canada
    Integr Environ Assess Manag 6:641-52. 2010
    ..biota sediment accumulation factors (BSAFs) for polychlorinated biphenyls (total PCB) and polychlorinated dioxins-furans (PCDD/Fs) in the Canadian Great Lakes using measured lake sediment and fish tissue concentrations in 4 fish ..
  93. ncbi Isofurans: novel products of lipid peroxidation that define the occurrence of oxidant injury in settings of elevated oxygen tension
    Joshua P Fessel
    Department of Pharmacology, Vanderbilt University, Nashville, TN 37232 6602, USA
    Antioxid Redox Signal 7:202-9. 2005
    ....
  94. 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...
  95. 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
    ....
  96. 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...
  97. ncbi 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 ..
  98. 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 ..
  99. ncbi 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)...
  100. 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...
  101. 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...

Research Grants62

  1. 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, ..
  2. Dioxins and Male Pubertal Growth and Development
    Russ B Hauser; Fiscal Year: 2013
    ..In laboratory animals and limited human studies, dioxins, furans, PCBs and lead were shown to alter pubertal development and growth and affect adult testicular function...
  3. 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...
  4. POTENTIAL FOR ENVIRONMENTAL AND THERAPEUTIC AGENTS TO INDUCE IMMUNOTOXICITY
    Matthew Smith; Fiscal Year: 2012
    ..During this period we have conducted studies to examine the relative potencies of four brominated dioxins and furans as compared with their chlorinated counterparts...
  5. Novel Direct Approaches Toward Bioactive Heterocycles
    Vladimir Gevorgyan; Fiscal Year: 2013
    ..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 ..
  6. 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...
  7. 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...
  8. 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...
  9. HYBRID TANDEM MASS SPECTROMETRY OF PEPTIDE CONJUGATES
    KEVIN BALLARD; Fiscal Year: 1993
    ..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 ..
  10. 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 ..
  11. 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...
  12. 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 ..
  13. 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...
  14. 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...
  15. 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 ..
  16. STRATEGIES FOR THE SYNTHESIS OF ANTICANCER AGENTS
    Stephen Martin; Fiscal Year: 1992
    ..Finally, new applications of the use of furans and hydropyranones derived therefrom in asymmetric synthesis of acyclic arrays will be developed...
  17. FURAN-CARBONYL PHOTOCYCLOADDITIONS IN ORGANIC SYNTHESIS
    Stuart Schreiber; Fiscal Year: 1991
    ..of mechanistic considerations and preliminary findings the intramolecular photocycloaddition of 2-substituted furans is expected to result in an efficient route to highly unusual tricyclic ring systems...
  18. Synthesis of Macrolides, Steroids, Cyclopentanoids, etc.
    BARRY TROST; Fiscal Year: 2009
    ..These new synthetic methods apply to many structural types beyond those illustrated and constitutes a significant to gain access to complex molecular targets more easily. ..
  19. SYNTHESIS OF MOLECULES OF BIOLOGICAL INTEREST
    Philip Magnus; Fiscal Year: 1980
    ..We have been developing new methods of making furans based on an allene reagent. The fragmentation of cyclic enones mediated by silicon is being investigated...
  20. Synthesis of Tumor Inhibitory Marine Natural Products
    James Marshall; Fiscal Year: 2004
    ..The main chemical issues to be addressed include the control of stereochemistry by means of chiral organometal chemistry and the design of new and efficient routes to structurally novel natural products. ..
  21. SYNTHESIS OF ANNONACEOUS ACETOGENINS AND ANALOGUES
    James Marshall; Fiscal Year: 2001
    ..The synthetic approach will employ chiral allylic and allenic organometal reagents to introduce stereogenic centers with concurrent formation of carbon-carbon bonds. ..
  22. DEVELOPMENT OF LIGAND ASSISTED ASYMMETRIC SYNTHESES
    Arun Ghosh; Fiscal Year: 2001
    ..Besides the broad range of scope and generality, this line of research will provide excellent opportunities to teach and train graduate and undergraduate students in the laboratory. ..
  23. DESIGN AND SYNTHESIS OF NONPEPTIDE PROTEASE INHIBITORS
    Arun K Ghosh; Fiscal Year: 2010
    ..This research integrates organic synthesis, protein-ligand x-ray crystallography, molecular modeling and in-depth virus and cell-biological studies to design the next generation of HIV-1 protease inhibitors. ..
  24. 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...
  25. SYNTHESIS OF FUSED HETEROCYCLIC COMPOUNDS
    Albert Padwa; Fiscal Year: 2002
    ..The generation of biologically active compounds by new synthetic methods remains an important part of both health related and chemical research. ..
  26. TOTAL SYNTHESIS OF AZADIRACHTIN
    K Nicolaou; Fiscal Year: 2008
    ..The proposed work is expected to impact the general areas of pharmaceutical and agricultural research, and infectious diseases in particular, through discoveries in synthetic organic chemistry and chemical biology. ..
  27. SYNTHESIS OF ANTICANCER AGENTS
    K C Nicolaou; Fiscal Year: 2010
    ..abstract_text> ..
  28. PHYSIOLOGICALLY ACTIVE NATURAL PRODUCTS
    Douglass Taber; Fiscal Year: 2007
    ..In the course of these investigations, new molecular reactivity will be developed that will substantially shorten current routes to polycyclic natural products and drug candidates. ..
  29. ANTI-VIRAL TREATMENT OF DEVELOPING BOVINE EMBRYOS
    Maurice Givens; Fiscal Year: 2002
    ....
  30. TOTAL SYNTHESIS OF NATURAL PRODUCTS
    K Nicolaou; Fiscal Year: 2002
    ..3] sigmatropic rearrangement and a radical based ring closure to form the bicyclic skeleton. ..
  31. TOTAL SYNTHESIS OF APOPTOLIDIN
    K Nicolaou; Fiscal Year: 2004
    ..The proposed work is expected to have significant impact in the area of cancer chemotherapy and should provide enabling technologies and tools for biology and medicine. ..
  32. Enabling Technologies for Combinatorial Chemistry
    K Nicolaou; Fiscal Year: 2005
    ..abstract_text> ..
  33. CO-CARCINOGENIC ACTIVITY OF NITROSAMINE METABOLITES
    Lisa Peterson; Fiscal Year: 2006
    ..In addition, this mechanism is likely applicable to other unsymmetric nitrosamines as well as carcinogenic mixtures such as tobacco smoke, a known human carcinogen. ..
  34. Role of O6-alkylguanine in nitrosamine-induced cancers
    Lisa Peterson; Fiscal Year: 2009
    ..These studies will set the stage for a molecular epidemiological study to determine whether individuals who are unable to repair this mutagenic adduct are at increased risk of tobacco-related cancers. ..
  35. Catalytic Processes for Selective Organic Synthesis
    GARY MOLANDER; Fiscal Year: 2005
    ..4) Carbometalation/cyclization reactions will be explored utilizing organochromium species. 5) Ligands and catalytic systems designed for asymmetric synthesis will be explored. ..
  36. Agilent 5973 GC/MS System
    GARY MOLANDER; Fiscal Year: 2002
    ..Our current lack of such instrumentation negatively affects the ability to carry out many of these studies. This critical capability, in the form of an instrument for everyday analysis, is urgently needed. ..
  37. TUMOR REMISSION--TAXOL AND CLOSE ANALOGS VIA SYNTHESIS
    LEO PAQUETTE; Fiscal Year: 2003
    ..These include, but are not limited to, the 1-deoxy, D-homo-, 2-desmethyl, and 12-methylene derivatives, in addition to the D-ring invertomer and the C-nor isomer. ..
  38. Micromass LCT Mass Spectrometer
    MICHAEL CRIMMINS; Fiscal Year: 2004
    ..The major users group is highly dependent on rapid turn around mass spectral data. Since there is currently no Departmental mass spectrometry facility, the research programs of the major users have been seriously hampered for some time. ..
  39. ASYMMETRIC SYNTHESIS OF NOVEL NATURAL PRODUCTS
    MICHAEL CRIMMINS; Fiscal Year: 2006
    ..Synthesis of the biologically active agents guanacastepene, and SCH 351448 will also be pursued. ..
  40. ASYMMETRIC SYNTHESIS OF ANTITUMOR AGENTS
    MICHAEL CRIMMINS; Fiscal Year: 2005
    ..Laulimalide stimulates tubulin polymerization more effectively than paclitaxel. Laulimalide is a representative of a new class of microtubule stabilizing agents with promise for therapeutic potential. ..
  41. Asymmetric Synthesis of Cytotoxic Natural Products
    Robert Coleman; Fiscal Year: 2005
    ..abstract_text> ..
  42. Single Agents with Designed Combination Chemotherapy Potential
    Aleem Gangjee; Fiscal Year: 2010
    ..abstract_text> ..
  43. SARS-CoV S Protein Receptor-binding Domain-based Vaccines
    Shibo Jiang; Fiscal Year: 2010
    ..The long-term goal of this project is to develop highly effective and safe subunit vaccines for protecting at-risk populations from SARS-CoV infection or bioterrorism attack. ..
  44. Rational Design of HIV Fusion Inhibitors Targeting gp41
    Shibo Jiang; Fiscal Year: 2010
    ..Therefore, this research is relevant to public health. ..
  45. Antitumor Antimitotics That Reverse Tumor Resistance
    Aleem Gangjee; Fiscal Year: 2010
    ..The study will also further define the mechanism of action of the novel series and could afford agents for clinical use. ..
  46. STRUCTURE BASED ANALOGS AS ANTIOPPORTUNISTIC AGENTS
    Aleem Gangjee; Fiscal Year: 2001
    ..The analogues synthesized will also be submitted for screening against tuberculosis (NIAID) parasitic diseases (WHO) and tumor cells in culture (NCI). ..
  47. Third Generation Antiopportunistic Agents
    Aleem Gangjee; Fiscal Year: 2003
    ..Screening against tuberculosis (NIAID) and tumor cells in culture (NCI) is also proposed. ..
  48. Novel, P. jirovecii Specific Antipneumocystis Agents
    Aleem Gangjee; Fiscal Year: 2009
    ..These agents could be used alone or in combination to treat PCP thus providing novel agents against a new target. ..
  49. NEW STRATEGIES FOR GLYCOCONJUGATE SYNTHESIS
    Frank McDonald; Fiscal Year: 2005
    ....
  50. Synthesis of the myrmicarin family of natural products
    Scott Snyder; Fiscal Year: 2005
    ....
  51. A General Synthetic Route to Glycosidase Inhibitors
    Aaron Aponick; Fiscal Year: 2006
    ....
  52. NOVEL NONINDUCIBLE THYMIDYLATE SYNTHASE INHIBITORS
    Aleem Gangjee; Fiscal Year: 2004
    ....
  53. Azinomycins - Total Synthesis and Mechanism of Action
    Robert Coleman; Fiscal Year: 2007
    ..abstract_text> ..
  54. Novel Single, Dual and Multitargeted Inhibitors of RTKs
    Aleem Gangjee; Fiscal Year: 2007
    ..abstract_text> ..
  55. Cell Growth Inhibiton and Estrogen Action
    Barry Markaverich; Fiscal Year: 2004
    ..The proposed studies should precisely define specific effects of MeHPLA and bioflavonoids on chromatin structure and function, growth related gene transcription and cellular proliferation in normal and malignant cells. ..
  56. A NOVEL ENDOCRINE DISRUPTING AGENT AND BREAST CANCER
    Barry Markaverich; Fiscal Year: 2007
    ..The proposed studies represent a critical step in defining target pathways for ultimately determining the mechanism of action of these compounds. ..
  57. SYNTHESIS OF THE TEDANOLIDES, CYTOTOXIC POLYPROPIONATES
    Michael Jung; Fiscal Year: 2003
    ....
  58. Occupational risk factors for NHL and NHL subtypes: an InterLymph-based analysis
    ANDREA MANNETJE; Fiscal Year: 2008
    ..This large study conducted by an international team of expert collaborators will provide sufficient study power to reach the outlined aims and contribute to the knowledge of the etiology of NHL. [unreadable] [unreadable] [unreadable]..
  59. Anti-HIV-1 Composite Cellulose Acetate Phthalate Film
    Shibo Jiang; Fiscal Year: 2008
    ....
  60. Alpha Folate Receptor Mediated GARFTase Inhibitors as Selective Antitumor Agents
    Aleem Gangjee; Fiscal Year: 2010
    ....