indenes

Summary

Summary: A family of fused-ring hydrocarbons isolated from coal tar that act as intermediates in various chemical reactions and are used in the production of coumarone-indene resins.

Top Publications

  1. pmc COI1 is a critical component of a receptor for jasmonate and the bacterial virulence factor coronatine
    Leron Katsir
    Department of Energy Plant Research Laboratory, Michigan State University, East Lansing, MI 48824, USA
    Proc Natl Acad Sci U S A 105:7100-5. 2008
  2. ncbi The phytotoxin coronatine contributes to pathogen fitness and is required for suppression of salicylic acid accumulation in tomato inoculated with Pseudomonas syringae pv. tomato DC3000
    Srinivasa Rao Uppalapati
    Department of Entomology and Plant Pathology, Oklahoma State University, Stillwater 74078, USA
    Mol Plant Microbe Interact 20:955-65. 2007
  3. ncbi Virulence systems of Pseudomonas syringae pv. tomato promote bacterial speck disease in tomato by targeting the jasmonate signaling pathway
    Youfu Zhao
    Department of Energy Plant Research Laboratory, Michigan State University, East Lansing, MI 48824, USA
    Plant J 36:485-99. 2003
  4. ncbi The phytotoxin coronatine and methyl jasmonate impact multiple phytohormone pathways in tomato
    Srinivasa Rao Uppalapati
    Department of Entomology and Plant Pathology, Oklahoma State University, Stillwater, OK 74078, USA
    Plant J 42:201-17. 2005
  5. pmc A critical role of two positively charged amino acids in the Jas motif of Arabidopsis JAZ proteins in mediating coronatine- and jasmonoyl isoleucine-dependent interactions with the COI1 F-box protein
    Maeli Melotto
    Department of Energy, Plant Research Laboratory, Michigan State University, East Lansing, MI 48824, USA
    Plant J 55:979-88. 2008
  6. ncbi Analysis of Arabidopsis JAZ gene expression during Pseudomonas syringae pathogenesis
    Agnes J Demianski
    Department of Biology, Washington University, St Louis, MO 63130, USA
    Mol Plant Pathol 13:46-57. 2012
  7. ncbi Novel indenoisoquinolines NSC 725776 and NSC 724998 produce persistent topoisomerase I cleavage complexes and overcome multidrug resistance
    Smitha Antony
    Laboratory of Molecular Pharmacology, National Cancer Institute, NIH, Bethesda, MD 20892 4255, USA
    Cancer Res 67:10397-405. 2007
  8. pmc A virus-induced gene silencing screen identifies a role for Thylakoid Formation1 in Pseudomonas syringae pv tomato symptom development in tomato and Arabidopsis
    Tamding Wangdi
    Plant Biology Division, Samuel Roberts Noble Foundation, Ardmore, Oklahoma 73401, USA
    Plant Physiol 152:281-92. 2010
  9. ncbi Differential induction of topoisomerase I-DNA cleavage complexes by the indenoisoquinoline MJ-III-65 (NSC 706744) and camptothecin: base sequence analysis and activity against camptothecin-resistant topoisomerases I
    Smitha Antony
    Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute NIH, 37 Convent Drive, Bethesda, MD 20892 4255, USA
    Cancer Res 63:7428-35. 2003
  10. ncbi A versatile partner of eukaryotic protein complexes that is involved in multiple biological processes: Kti11/Dph3
    Christian Bär
    Biologicum, Institut fur Genetik, Martin Luther Universitat Halle Wittenberg, Weinbergweg 10, D 06120 Halle Saale, Germany
    Mol Microbiol 69:1221-33. 2008

Research Grants

  1. Pilot-Scale Heterocyclic and Carbocyclic Libraries for High Throughout Screening
    RICHARD LAROCK; Fiscal Year: 2009
  2. Synthesis of Medicinally Important Heterocycles
    RICHARD LAROCK; Fiscal Year: 2007
  3. DAYTIME SLEEPINESS--PREVALENCE, CONSEQUENCES, AND RISKS
    Thomas Roth; Fiscal Year: 2003
  4. PARS inhibitor for cardiac allotransplantation
    Prakash Jagtap; Fiscal Year: 2002
  5. Novel PARS inhibitor for therapy of colitis
    Prakash Jagtap; Fiscal Year: 2002
  6. Novel antioxidant catalyst for transplant rejection
    Prakash Jagtap; Fiscal Year: 2003
  7. Novel Single, Dual and Multitargeted Inhibitors of RTKs
    Aleem Gangjee; Fiscal Year: 2007
  8. Light Stimulation of Luteinizing Hormone
    DANIEL KRIPKE; Fiscal Year: 2006
  9. Melatonin Randomized Trial in Insomnia in the Elderly
    Nalaka Gooneratne; Fiscal Year: 2006
  10. b-TrCP E3 Ligase in CLL
    Benjamin Nicholson; Fiscal Year: 2006

Detail Information

Publications208 found, 100 shown here

  1. pmc COI1 is a critical component of a receptor for jasmonate and the bacterial virulence factor coronatine
    Leron Katsir
    Department of Energy Plant Research Laboratory, Michigan State University, East Lansing, MI 48824, USA
    Proc Natl Acad Sci U S A 105:7100-5. 2008
    ..These findings demonstrate that COI1 is a critical component of the JA receptor and that COR exerts its virulence effects by functioning as a potent agonist of this receptor system...
  2. ncbi The phytotoxin coronatine contributes to pathogen fitness and is required for suppression of salicylic acid accumulation in tomato inoculated with Pseudomonas syringae pv. tomato DC3000
    Srinivasa Rao Uppalapati
    Department of Entomology and Plant Pathology, Oklahoma State University, Stillwater 74078, USA
    Mol Plant Microbe Interact 20:955-65. 2007
    ....
  3. ncbi Virulence systems of Pseudomonas syringae pv. tomato promote bacterial speck disease in tomato by targeting the jasmonate signaling pathway
    Youfu Zhao
    Department of Energy Plant Research Laboratory, Michigan State University, East Lansing, MI 48824, USA
    Plant J 36:485-99. 2003
    ....
  4. ncbi The phytotoxin coronatine and methyl jasmonate impact multiple phytohormone pathways in tomato
    Srinivasa Rao Uppalapati
    Department of Entomology and Plant Pathology, Oklahoma State University, Stillwater, OK 74078, USA
    Plant J 42:201-17. 2005
    ....
  5. pmc A critical role of two positively charged amino acids in the Jas motif of Arabidopsis JAZ proteins in mediating coronatine- and jasmonoyl isoleucine-dependent interactions with the COI1 F-box protein
    Maeli Melotto
    Department of Energy, Plant Research Laboratory, Michigan State University, East Lansing, MI 48824, USA
    Plant J 55:979-88. 2008
    ....
  6. ncbi Analysis of Arabidopsis JAZ gene expression during Pseudomonas syringae pathogenesis
    Agnes J Demianski
    Department of Biology, Washington University, St Louis, MO 63130, USA
    Mol Plant Pathol 13:46-57. 2012
    ..Thus, JAZ10 is a negative regulator of both JA signalling and disease symptom development...
  7. ncbi Novel indenoisoquinolines NSC 725776 and NSC 724998 produce persistent topoisomerase I cleavage complexes and overcome multidrug resistance
    Smitha Antony
    Laboratory of Molecular Pharmacology, National Cancer Institute, NIH, Bethesda, MD 20892 4255, USA
    Cancer Res 67:10397-405. 2007
    ..These gamma-H2AX foci were detectable at pharmacologically relevant doses for up to 24 h and thus could be used as biomarkers for clinical trials (phase 0)...
  8. pmc A virus-induced gene silencing screen identifies a role for Thylakoid Formation1 in Pseudomonas syringae pv tomato symptom development in tomato and Arabidopsis
    Tamding Wangdi
    Plant Biology Division, Samuel Roberts Noble Foundation, Ardmore, Oklahoma 73401, USA
    Plant Physiol 152:281-92. 2010
    ..In conclusion, our results show that the virus-induced gene silencing-based forward genetic screen has the potential to identify new players in COR signaling and disease-associated necrotic cell death...
  9. ncbi Differential induction of topoisomerase I-DNA cleavage complexes by the indenoisoquinoline MJ-III-65 (NSC 706744) and camptothecin: base sequence analysis and activity against camptothecin-resistant topoisomerases I
    Smitha Antony
    Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute NIH, 37 Convent Drive, Bethesda, MD 20892 4255, USA
    Cancer Res 63:7428-35. 2003
    ..This study shows the specific molecular interactions of MJ-III-65 with top1 and demonstrates that MJ-III-65 is a potentially useful top1 inhibitor that enhances and traps top1 cleavage sites not sensitive to CPTs...
  10. ncbi A versatile partner of eukaryotic protein complexes that is involved in multiple biological processes: Kti11/Dph3
    Christian Bär
    Biologicum, Institut fur Genetik, Martin Luther Universitat Halle Wittenberg, Weinbergweg 10, D 06120 Halle Saale, Germany
    Mol Microbiol 69:1221-33. 2008
    ..It encodes a C-terminal Kti11 truncation that almost entirely abolishes Elongator interaction without affecting association with Kti13, another Kti11 partner protein...
  11. pmc A novel norindenoisoquinoline structure reveals a common interfacial inhibitor paradigm for ternary trapping of the topoisomerase I-DNA covalent complex
    Christophe Marchand
    Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, Building 37, Room 5068, Bethesda, MD 20892 4255, USA
    Mol Cancer Ther 5:287-95. 2006
    ..Stabilization of such conformational states results in uncompetitive inhibition and exemplifies the relevance of screening for ligands and drugs that stabilize ("trap") these macromolecular complexes...
  12. ncbi SGT1 contributes to coronatine signaling and Pseudomonas syringae pv. tomato disease symptom development in tomato and Arabidopsis
    Srinivasa Rao Uppalapati
    Plant Biology Division, The Samuel Roberts Noble Foundation Inc, Ardmore, OK 73401, USA
    New Phytol 189:83-93. 2011
    ..SGT1 is therefore a component of the COR/JA-mediated signal transduction pathway...
  13. ncbi BZYX, a novel acetylcholinesterase inhibitor, significantly improved chemicals-induced learning and memory impairments on rodents and protected PC12 cells from apoptosis induced by hydrogen peroxide
    Jing Zhang
    Institute of Pharmacology and Toxicology, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, China
    Eur J Pharmacol 613:1-9. 2009
    ..It is hopeful that BZYX becomes a potential candidate for use in the intervention for neurodegenerative diseases...
  14. ncbi NTRC and chloroplast-generated reactive oxygen species regulate Pseudomonas syringae pv. tomato disease development in tomato and Arabidopsis
    Yasuhiro Ishiga
    Plant Biology Division, Samuel Roberts Noble Foundation, Ardmore, OK 73401, USA
    Mol Plant Microbe Interact 25:294-306. 2012
    ....
  15. ncbi Identification and characterization of a well-defined series of coronatine biosynthetic mutants of Pseudomonas syringae pv. tomato DC3000
    David M Brooks
    Department of Biology, Washington University, St Louis, MO 63130, USA
    Mol Plant Microbe Interact 17:162-74. 2004
    ..thaliana is caused by the absence of the intact COR toxin. This is the first study to use biochemically and genetically defined COR mutants to address the role of COR in pathogenesis...
  16. pmc Zebrafish chemical screening reveals an inhibitor of Dusp6 that expands cardiac cell lineages
    Gabriela Molina
    Department of Microbiology and Molecular Genetics, University of Pittsburgh, Pittsburgh, Pennsylvania, USA
    Nat Chem Biol 5:680-7. 2009
    ..This study highlights the power of in vivo zebrafish chemical screens to identify new compounds targeting Dusp6, a component of the FGF signaling pathway that has eluded traditional high-throughput in vitro screens...
  17. pmc A chemical genomic screen in Saccharomyces cerevisiae reveals a role for diphthamidation of translation elongation factor 2 in inhibition of protein synthesis by sordarin
    Javier Botet
    Departamento de Microbiologia y Genetica, Instituto de Microbiologia Bioquimica, CSIC and Universidad de Salamanca, Salamanca, Spain
    Antimicrob Agents Chemother 52:1623-9. 2008
    ..Our results underscore the importance of the powerful genomic tools developed in yeast (Saccharomyces cerevisiae) to more comprehensively understanding the cellular mechanisms involved in the response to therapeutic agents...
  18. ncbi Recent developments in the medicinal chemistry of cannabimimetic indoles, pyrroles and indenes
    J W Huffman
    H L Hunter Chemistry Laboratory, Clemson University, Clemson, South Carolina 29634 0973, USA
    Curr Med Chem 12:1395-411. 2005
    ..On the basis of a proposed pharmacophore for the cannabimimetic indoles, a series of pyrroles and indenes were developed, some of which are potent cannabinoids. SAR for several series of pyrroles have been developed...
  19. ncbi Potent antitumor bifunctional DNA alkylating agents, synthesis and biological activities of 3a-aza-cyclopenta[a]indenes
    Rajesh Kakadiya
    Institute of Biomedical Sciences, Academia Sinica, Taipei 11529, Taiwan
    Bioorg Med Chem 17:5614-26. 2009
    ..The current studies suggested that these agents are promising candidates for preclinical studies...
  20. ncbi Spirolactone iridoids might be responsible for the antileishmanial activity of a Peruvian traditional remedy made with Himatanthus sucuuba (Apocynaceae)
    D Castillo
    Instituto de Medicina Tropical Alexander von Humboldt, Universidad Peruana Cayetano Heredia UPCH, Av Honorio Delgado 430, SMP, Lima, Peru
    J Ethnopharmacol 112:410-4. 2007
    ..9 and 1 microM, respectively). These findings validate the traditional use of Himatanthus sucuuba in the treatment of cutaneous leishmaniasis (Uta) in Peru...
  21. pmc Domain movements of elongation factor eEF2 and the eukaryotic 80S ribosome facilitate tRNA translocation
    Christian M T Spahn
    Wadsworth Center, Health Research Inc, Howard Hughes Medical Institute, Albany, NY 12201 0509, USA
    EMBO J 23:1008-19. 2004
    ..sordarin complex that, in contrast to Escherichia coli 70S ribosomes, is also present in vacant 80S ribosomes. A model is suggested, according to which the RSR is part of a mechanism for moving the tRNAs during the translocation reaction...
  22. ncbi A bioactive spirolactone iridoid and triterpenoids from Himatanthus sucuuba
    C A Wood
    Department of Chemistry and Biochemistry, University of Massachusetts-Dartmouth, 02747, USA
    Chem Pharm Bull (Tokyo) 49:1477-8. 2001
    ....
  23. ncbi Structures of three classes of anticancer agents bound to the human topoisomerase I-DNA covalent complex
    Bart L Staker
    deCODE BioStructures, 7869 NE Day Road West, Bainbridge Island, Washington 98110, USA
    J Med Chem 48:2336-45. 2005
    ..These new X-ray structures explain how very different molecules can stabilize top1-DNA covalent complexes and will aid the rational design of completely novel structural classes of anticancer drugs...
  24. ncbi Binding of isotryptamines and indenes at h5-HT6 serotonin receptors
    Renata Kolanos
    Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond, VA 23298 0540, USA
    Bioorg Med Chem Lett 15:1987-91. 2005
    ..The affinity of 3-benzyl-N(1)-(N,N-dimethylaminoethyl)indole (5, K(i)=32nM) and 1-benzyl-3-(N,N-dimethylaminoethyl)indene (11, K(i)=3nM) indicates that the indolic nitrogen atom is not essential for binding...
  25. pmc The plant innate immunity response in stomatal guard cells invokes G-protein-dependent ion channel regulation
    Wei Zhang
    Biology Department, Penn State University, University Park, PA 16802 5301, USA
    Plant J 56:984-96. 2008
    ..These new findings provide insights into the largely elusive signaling process underlying PTI-associated guard cell responses...
  26. ncbi Effect of ramelteon (TAK-375), a selective MT1/MT2 receptor agonist, on motor performance in mice
    Masaomi Miyamoto
    Pharmacology Research Laboratories III, Takeda Pharmaceutical Company Limited, Osaka 532 8686, Japan
    Neurosci Lett 402:201-4. 2006
    ..o.), treatment with melatonin and N-acetyl-5-HT exacerbated the impairment by diazepam. Ramelteon had no significant effect on the diazepam-induced impairment of motor coordination...
  27. ncbi The sleep-promoting action of ramelteon (TAK-375) in freely moving cats
    Masaomi Miyamoto
    Pharmacology Research Laboratories I, Takeda Pharmaceutical Company Ltd, Osaka, Japan
    Sleep 27:1319-25. 2004
    ..Ramelteon (TAK-375) is an MT1/MT2 receptor agonist being studied for the treatment of insomnia and circadian rhythm sleep disorders. We compared the behavioral effects of ramelteon and exogenous melatonin in freely moving cats...
  28. pmc Evaluation of the efficacy and safety of ramelteon in subjects with chronic insomnia
    Gary Zammit
    Clinilabs Sleep Disorders Institute, New York, NY 10025, USA
    J Clin Sleep Med 3:495-504. 2007
    ..To evaluate efficacy and safety of ramelteon (MT1/MT2-receptor [corrected] agonist) in subjects with chronic primary insomnia...
  29. ncbi Effects of ramelteon (TAK-375) on nocturnal sleep in freely moving monkeys
    Nobuhito Yukuhiro
    Pharmacology Research Laboratories I, Pharmaceutical Research Division, Takeda Pharmaceutical Company Ltd, Osaka 532 8686, Japan
    Brain Res 1027:59-66. 2004
    ..The EEG power spectra of zolpidem were qualitatively different from that of naturally occurring physiological sleep. Results of the present study support the investigation of ramelteon as a sleep-promoting agent in humans...
  30. ncbi Drug Insight: the use of melatonergic agonists for the treatment of insomnia-focus on ramelteon
    Seithikurippu R Pandi-Perumal
    Comprehensive Center for Sleep Medicine, Division of Pulmonary, Critical Care and Sleep Medicine, Mount Sinai School of Medicine, New York, NY 10029, USA
    Nat Clin Pract Neurol 3:221-8. 2007
    ..Although ramelteon's metabolism and pharmacokinetics differ from those of melatonin, its safety seems to be sufficient for short-term application. Its long-term effects remain to be determined...
  31. ncbi Ramelteon (TAK-375) accelerates reentrainment of circadian rhythm after a phase advance of the light-dark cycle in rats
    Keisuke Hirai
    Pharmacology Research Laboratories I, Pharmaceutical Research Division, Takeda Pharmaceutical Company Ltd, Osaka, Japan
    J Biol Rhythms 20:27-37. 2005
    ....
  32. ncbi Acute and chronic effects of ramelteon in rhesus monkeys (Macaca mulatta): dependence liability studies
    Charles P France
    Department of Pharmacology, University of Texas Health Science Center, San Antonio, TX 78229 3900, USA
    Behav Neurosci 120:535-41. 2006
    ..These findings suggest that ramelteon is not likely to have benzodiazepine-like abuse or dependence liability...
  33. ncbi Melatonergic drugs in clinical practice
    Rudiger Hardeland
    Johann Friedrich Blumenbach Institute of Zoology and Anthropology, Universityof Göttingen, Gottingen, Germany
    Arzneimittelforschung 58:1-10. 2008
    ..g., on reproductive functions. According to current data, both compounds seem to be safe during short-term treatment..
  34. ncbi Ramelteon (TAK-375), a selective MT1/MT2-receptor agonist, reduces latency to persistent sleep in a model of transient insomnia related to a novel sleep environment
    Thomas Roth
    Sleep Disorders and Research Center, Henry Ford Hospital, Detroit, MI 48202, USA
    Sleep 28:303-7. 2005
    ..Evaluate the efficacy of ramelteon, an MT/1MT2-receptor agonist, for the treatment of transient insomnia in healthy adults...
  35. ncbi Ramelteon: a novel hypnotic lacking abuse liability and sedative adverse effects
    Matthew W Johnson
    Department of Psychiatry and Behavioral Sciences, The Johns Hopkins University School of Medicine, Baltimore, MD 21224, USA
    Arch Gen Psychiatry 63:1149-57. 2006
    ..Ramelteon is a novel MT1 and MT2 melatonin receptor selective agonist recently approved for insomnia treatment. Most approved insomnia medications have potential for abuse and cause motor and cognitive impairment...
  36. ncbi An efficacy, safety, and dose-response study of Ramelteon in patients with chronic primary insomnia
    Milton Erman
    Pacific Sleep Medicine Services, San Diego, CA 92121, USA
    Sleep Med 7:17-24. 2006
    ..To evaluate the efficacy, safety, and dose response of Ramelteon, a novel highly selective MT1/MT2 receptor agonist, in patients with chronic primary insomnia...
  37. ncbi Disposition kinetics and tolerance of escalating single doses of ramelteon, a high-affinity MT1 and MT2 melatonin receptor agonist indicated for treatment of insomnia
    Aziz Karim
    Takeda Global Research and Development Center, Inc, 475 Half Day Road, Lincolnshire, IL 60069, USA
    J Clin Pharmacol 46:140-8. 2006
    ..Digit Symbol Substitution Test and visual analog scale alertness scores were similar across all dose groups and did not differ from placebo. All adverse events were mild or moderate and resolved before study completion...
  38. ncbi Effects of ramelteon on patient-reported sleep latency in older adults with chronic insomnia
    Thomas Roth
    Sleep Disorders and Research Center, Henry Ford Hospital, 2799 West Grand Boulevard, CFP 3, Detroit, MI 48202, USA
    Sleep Med 7:312-8. 2006
    ..To assess the efficacy and safety of ramelteon, a selective MT(1)/MT(2) receptor agonist, for chronic insomnia treatment...
  39. ncbi Neurochemical properties of ramelteon (TAK-375), a selective MT1/MT2 receptor agonist
    Koki Kato
    Pharmacology Research Laboratories I, Pharmaceutical Research Division, Takeda Pharmaceutical Company Ltd, Osaka 532 8686, Japan
    Neuropharmacology 48:301-10. 2005
    ..Taken together, these results indicate that ramelteon is a potent and highly selective agonist of MT1/MT2 melatonin receptors...
  40. ncbi Preparation and pharmacological characterization of trans-2-amino-5(6)-fluoro-6(5)-hydroxy-1-phenyl-2,3-dihydro-1H-indenes as D2-like dopamine receptor agonists
    Antonio Di Stefano
    Dipartimento di Scienze del Farmaco, Universita G D Annunzio, Via dei Vestini 31, 66100 Chieti, Italy
    J Med Chem 48:2646-54. 2005
    The present work reports the synthesis of trans-2-amino-5(6)-fluoro-6(5)-hydroxy-1-phenyl-2,3-dihydro-1H-indenes (4a-f, 5a-f) as a continuation of our studies to better understand the significance of the halo substituent in the trans-1-..
  41. ncbi The phytotoxin coronatine induces light-dependent reactive oxygen species in tomato seedlings
    Yasuhiro Ishiga
    127 Noble Research Center, Department of Entomology and Plant Pathology, Oklahoma State University, Stillwater, OK 74078, USA
    New Phytol 181:147-60. 2009
    ..In conclusion, these results demonstrate a role for COR-induced effects on photosynthetic machinery and ROS in modulating necrotic cell death during bacterial speck disease of tomato...
  42. ncbi Synthesis and evaluation of heteroaryl-substituted dihydronaphthalenes and indenes: potent and selective inhibitors of aldosterone synthase (CYP11B2) for the treatment of congestive heart failure and myocardial fibrosis
    Marieke Voets
    8 2 Pharmaceutical and Medicinal Chemistry, Saarland University, P O Box 15 11 50, D 66041 Saarbruecken, Germany
    J Med Chem 49:2222-31. 2006
    In this study, the synthesis and biological evaluation of heteroaryl-substituted dihydronaphthalenes and indenes (1-16) is described...
  43. pmc Synthesis and evaluation of indenoisoquinoline topoisomerase I inhibitors substituted with nitrogen heterocycles
    Muthukaman Nagarajan
    Department of Medicinal Chemistry and Molecular Pharmacology, and the Purdue Cancer Center, School of Pharmacy and Pharmaceutical Sciences, Purdue University, West Lafayette, Indiana 47907, USA
    J Med Chem 49:6283-9. 2006
    ....
  44. ncbi Pathogenicity of Pseudomonas syringae pv. tomato on tomato seedlings: phenotypic and gene expression analyses of the virulence function of coronatine
    Srinivasa Rao Uppalapati
    Department of Entomology and Plant Pathology, Oklahoma State University, Stillwater, OK 74078, USA
    Mol Plant Microbe Interact 21:383-95. 2008
    ..The seedling assay can be used in high-throughput screens for the identification of molecular targets for COR and for the identification of genes involved in pathogenesis...
  45. ncbi Further studies on imidazo[4,5-b]pyridine AT1 angiotensin II receptor antagonists. Effects of the transformation of the 4-phenylquinoline backbone into 4-phenylisoquinolinone or 1-phenylindene scaffolds
    Andrea Cappelli
    Dipartimento Farmaco Chimico Tecnologico and European Research Centre for Drug Discovery and Development, Universita di Siena, Via A Moro, 53100 Siena, Italy
    J Med Chem 49:6451-64. 2006
    ..Finally, a set of 34 AT(1) receptor antagonists was used as a new test for the evaluation of the predictive capability of the previously published qualitative and quantitative pharmacophore models...
  46. pmc Investigation of the lactam side chain length necessary for optimal indenoisoquinoline topoisomerase I inhibition and cytotoxicity in human cancer cell cultures
    Andrew Morrell
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmaceutical Sciences, and the Purdue Cancer Center, Purdue University, West Lafayette, Indiana 47907, USA
    J Med Chem 50:2040-8. 2007
    ..Using these lengths, analogues were prepared with the amino group and portions of the linker replaced by a pyridine ring. A three-carbon spacer within the pyridine series still demonstrated potent topoisomerase I inhibition...
  47. ncbi 1,4-Dihydroindeno[1,2-c]pyrazoles with acetylenic side chains as novel and potent multitargeted receptor tyrosine kinase inhibitors with low affinity for the hERG ion channel
    Jurgen Dinges
    Global Pharmaceutical Research and Development, Abbott Laboratories, 200 Abbott Park Road, Abbott Park, Illinois 60064 6217, USA
    J Med Chem 50:2011-29. 2007
    ..The selectivity profile for 8 and 90 revealed that both compounds are multitargeted receptor tyrosine kinase inhibitors with low nanomolar potencies against the members of the VEGFR and PDGFR kinase subfamilies...
  48. ncbi CorR regulates multiple components of virulence in Pseudomonas syringae pv. tomato DC3000
    Aswathy Sreedharan
    Department of Entomology and Plant Pathology, Oklahoma State University, Stillwater 74078, USA
    Mol Plant Microbe Interact 19:768-79. 2006
    ..A putative CorR-binding site was identified upstream of hrpL, and gel shift studies confirmed the binding of CorR to this region. These results indicate that corR directly impacts the expression of the hrp regulon in P. syringae...
  49. ncbi Neurosteroid analogues. 11. Alternative ring system scaffolds: gamma-aminobutyric acid receptor modulation and anesthetic actions of benz[f]indenes
    Jamie B Scaglione
    Department of Molecular Biology, Washington University School of Medicine, St Louis, Missouri 63110, USA
    J Med Chem 49:4595-605. 2006
    Benz[f]indenes are tricyclic compounds with a linear 6-6-5 fused carbocyclic ring system...
  50. ncbi 'Bridged' stilbene derivatives as selective cyclooxygenase-1 inhibitors
    Norbert Handler
    Department of Medicinal Chemistry, University of Vienna, Althanstrasse 14, A 1090 Vienna, Austria
    Bioorg Med Chem 15:6109-18. 2007
    ..Phenyl substituted 1,2-dihydronaphthalene derivatives and 1H-indene derivatives therefore represent a novel class of highly selective COX-1 inhibitors and land promising candidates for in vivo studies...
  51. pmc A systematic study of nitrated indenoisoquinolines reveals a potent topoisomerase I inhibitor
    Andrew Morrell
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmaceutical Sciences, and the Purdue Cancer Center, Purdue University, West Lafayette, IN 47907, USA
    J Med Chem 49:7740-53. 2006
    ....
  52. ncbi On the binding of indeno[1,2-c]isoquinolines in the DNA-topoisomerase I cleavage complex
    Xiangshu Xiao
    Department of Medicinal Chemistry and Molecular Pharmacology and the Purdue Cancer Center, School of Pharmacy and Pharmaceutical Sciences, Purdue University, West Lafayette, Indiana 47907, USA
    J Med Chem 48:3231-8. 2005
    ....
  53. ncbi Synthesis and biological evaluation of bisindenoisoquinolines as topoisomerase I inhibitors
    Muthukaman Nagarajan
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmaceutical Sciences and the Purdue Cancer Center, Purdue University, West Lafayette, Indiana 47907, USA
    J Med Chem 49:5129-40. 2006
    ....
  54. ncbi Optimization of the indenone ring of indenoisoquinoline topoisomerase I inhibitors
    Andrew Morrell
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmaceutical Sciences, Purdue Cancer Center, Purdue University, West Lafayette, Indiana 47907, USA
    J Med Chem 50:4388-404. 2007
    ..Interestingly, these functional groups coincide with established structure-activity relationships for the 11-position of camptothecin...
  55. ncbi Nitrated indenoisoquinolines as topoisomerase I inhibitors: a systematic study and optimization
    Andrew Morrell
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmaceutical Sciences, Purdue Cancer Center, Purdue University, West Lafayette, Indiana 47907, USA
    J Med Chem 50:4419-30. 2007
    ..As a result, this investigation has provided optimal Top1 inhibitors equipotent to camptothecin that demonstrate low nanomolar cytotoxicities toward cancer cells...
  56. ncbi Design, synthesis, and biological evaluation of indenoisoquinoline topoisomerase I inhibitors featuring polyamine side chains on the lactam nitrogen
    Muthukaman Nagarajan
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmacal Sciences, Purdue University, West Lafayette, IN 47907, USA
    J Med Chem 46:5712-24. 2003
    ..07 microM in the NIH human cancer cell culture screen, and topoisomerase I inhibitory activity comparable to that of camptothecin...
  57. ncbi Antifungal sordarins. part 3: synthesis and structure-activity relationships of 2',3'-fused oxirane derivatives
    Julia Castro
    GlaxoSmithKline, Research Department, Parque Tecnologico de Madrid, Severo Ochoa, 2 28760 Tres Cantos, Madrid, Spain
    Bioorg Med Chem Lett 12:1371-4. 2002
    ..Many of these derivatives exhibit high potency against Candida spp. In addition, sordarin manno epoxide derivative 6 presents in vivo therapeutic effect in mice and is considered a promising antifungal lead within this series...
  58. ncbi Synthesis of nitrated indenoisoquinolines as topoisomerase I inhibitors
    Andrew Morrell
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmacal Sciences, Purdue University, West Lafayette, IN 47907, USA
    Bioorg Med Chem Lett 14:3659-63. 2004
    ..The results indicate that these substances are a potent class of top1 inhibitors with sub-micromolar cytotoxicity mean graph midpoints (MGM) and top1 inhibition equal to camptothecin...
  59. ncbi Antifungal agents: mechanisms of action
    Frank C Odds
    Aberdeen Fungal Group, University of Aberdeen, Department of Molecular and Cell Biology, Institute of Medical Sciences, Aberdeen AB25 2ZD, UK
    Trends Microbiol 11:272-9. 2003
    ..This review describes the targets and mechanisms of action of all classes of antifungal agents in clinical use or with clinical potential...
  60. ncbi Identification of a broad-spectrum azasordarin with improved pharmacokinetic properties
    Michael H Serrano-Wu
    Bristol Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA
    Bioorg Med Chem Lett 13:1419-23. 2003
    ..Further investigation identified the 5'-i-Pr derivative 7b, which displays superior pharmacokinetic properties compared to other azasordarins...
  61. ncbi Synthesis and anticancer activity of simplified indenoisoquinoline topoisomerase I inhibitors lacking substituents on the aromatic rings
    Muthukaman Nagarajan
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmacal Sciences, Purdue University, West Lafayette, Indiana 47907, USA
    J Med Chem 47:5651-61. 2004
    ..The most cytotoxic of the presently synthesized indenoisoquinolines has a 4-amino-n-butyl group on the lactam nitrogen...
  62. ncbi Synthesis, structural reassignment, and biological activity of type B MAO inhibitors based on the 5H-indeno[1,2-c]pyridazin-5-one core
    Raphael Frederick
    Laboratoire de Chimie Biologique Structurale, Drug Design and Discovery Center, Facultes Universitaires N D de la Paix, 61 rue de Bruxelles, B 5000 Namur, Belgium
    J Med Chem 49:3743-7. 2006
    ..Investigation of the regioisomeric structures establishes that substitution of the 5H-indeno[1,2-c]pyridazin-5-one core at C(7) vs C(8) dramatically influences the MAO-inhibiting properties of these compounds...
  63. ncbi Multipoint recognition of catecholamines by hydrindacene-based receptors accompanied by the complexation-induced conformational switching
    Hidetoshi Kawai
    Division of Chemistry, Graduate School of Science, Hokkaido University, Sapporo 060 0810, Japan
    Chemistry 11:815-24. 2005
    ..On complex formation with adrenaline, the syn-conformer becomes dominant due to an intramolecular dipole-reversal effect in addition to multipoint hydrogen bonding...
  64. ncbi Synthesis and activity of analogues of the isoleucyl tRNA synthetase inhibitor SB-203207
    Curtis F Crasto
    Research School of Chemistry, Institute of Advanced Studies, Australian National University, Canberra, ACT 0200, Australia
    Bioorg Med Chem 11:2687-94. 2003
    ..In particular, a methionine derivative is 50-100 times more potent against methionyl tRNA synthetase than against any of the corresponding isoleucyl, leucyl, valyl, alanyl and prolyl synthetases...
  65. ncbi Cyanopyridyl containing 1,4-dihydroindeno[1,2-c]pyrazoles as potent checkpoint kinase 1 inhibitors: improving oral biovailability
    Yunsong Tong
    Cancer Research, Global Pharmaceutical R and D, R47S, AP10, Abbott Laboratories, 100 Abbott Park, Abbott Park, IL 60064, USA
    Bioorg Med Chem Lett 17:5665-70. 2007
    ..These compounds also possessed desirable cellular activity in potentiating doxorubicin and will serve as valuable tool compounds for in vivo evaluation of CHK-1 inhibitors to sensitize DNA-damaging agents...
  66. ncbi New ligands at the melatonin binding site MT(3)
    Marie Françoise Boussard
    Division de Chimie médicinale E, Institut de Recherches Servier, Suresnes, France
    Eur J Med Chem 41:306-20. 2006
    ....
  67. ncbi Synthesis and fungicidal activities of novel indene-substituted oxime ether strobilurins
    Song Tu
    Department of Chemical and Biochemical Engineering, College of Chemistry and Chemical Engineering, Xiamen University, Xiamen 361005, People s Republic of China
    J Agric Food Chem 56:5247-53. 2008
    ..Especially, the 6-methylindene-substituted compound 6p was identified as the most promising candidate for further study...
  68. ncbi An avenue to the sordarin core adaptable to analog synthesis
    Huan Liang
    Department of Chemistry, University of British Columbia, 2036 Main Mall, Vancouver, British Columbia V6T 1Z1, Canada
    Org Lett 9:4119-22. 2007
    ..Congeners of 1 constructed from 3 should permit detailed SAR investigations of the terpenoid core of the natural product...
  69. ncbi Synthesis and inotropic activity of 1-(O-aminoalkyloximes) of perhydroindene derivatives as simplified digitalis-like compounds acting on the Na(+),K(+)-ATPase
    Alberto Cerri
    Department of Medicinal Chemistry, Prassis Istituto di Ricerche Sigma Tau, Via Forlanini 3, 20019 Settimo Milanese MI, Italy
    J Med Chem 45:189-207. 2002
    ....
  70. ncbi Novel, orally bioavailable gamma-aminoamide CC chemokine receptor 2 (CCR2) antagonists
    Alexander Pasternak
    Department of Medicinal Chemistry and Department of Immunology Rheumatology, Merck Research Laboratories, Rahway, New Jersey 07065, USA
    J Med Chem 49:4801-4. 2006
    ..Antagonist 26 was shown to have good oral bioavailability in rats. Antagonist 37 had a CCR2 IC50 of 59 nM and excellent potency in a functional assay measuring inhibition of MCP-1 induced monocyte chemotaxis (IC50 of 41 nM)...
  71. ncbi Identification of (R)-1-(5-tert-butyl-2,3-dihydro-1H-inden-1-yl)-3-(1H-indazol-4-yl)urea (ABT-102) as a potent TRPV1 antagonist for pain management
    Arthur Gomtsyan
    Global Pharmaceutical Research and Development, Neuroscience Research, Abbott Laboratories, Abbott Park, IL 60064, USA
    J Med Chem 51:392-5. 2008
    ..Both the analgesic activity and drug-like properties of ( R)-7 support its advancement into clinical pain trials...
  72. ncbi Synthesis and structure-activity relationships of ring-opened 17-hydroxywortmannins: potent phosphoinositide 3-kinase inhibitors with improved properties and anticancer efficacy
    Arie Zask
    Wyeth Research, Pearl River, New York 10965, USA
    J Med Chem 51:1319-23. 2008
    ..Ring-opened analogues such as compound 13 containing basic amine groups have significantly increased PI3K inhibitory potency and greater efficacy in nude mouse xenograft assays...
  73. ncbi Structure-activity relationships of dimethindene derivatives as new M2-selective muscarinic receptor antagonists
    Thomas M Böhme
    Institute of Pharmacy, Johannes Gutenberg University of Mainz, Staudinger Weg 5, D 55099 Mainz, Germany
    J Med Chem 46:856-67. 2003
    A series of 2,3-disubstituted indenes, which are analogues of the widely used histamine H(1) receptor antagonist dimethindene, have been synthesized and studied as muscarinic and histamine receptor antagonists...
  74. ncbi First synthesis of enantiopure 1,6-difunctionalized dodecahydrobenz[f]indenes
    Jamie B Scaglione
    Department of Molecular Biology and Pharmacology, Washington University School of Medicine, 660 South Euclid Avenue, St Louis, MI 63110, USA
    J Org Chem 70:1089-92. 2005
    ..This allylic alcohol is then utilized in a Claisen rearrangement under Johnson's conditions to introduce a side chain that is further modified and cyclized to produce the benz[f]indene ring system...
  75. ncbi Site-directed mutagenesis of the temperature-sensing histidine protein kinase CorS from Pseudomonas syringae
    Angela V Smirnova
    Jacobs University Bremen, School of Engineering and Science, Campus Ring 1, Bremen, Germany
    FEMS Microbiol Lett 283:231-8. 2008
    ....
  76. ncbi Dinuclear manganese complexes containing chiral 1,4,7-triazacyclononane-derived ligands and their catalytic potential for the oxidation of olefins, alkanes, and alcohols
    Vladimir B Romakh
    Institut de Chimie, Universite de Neuchatel, CH 2009 Neuchatel, Switzerland
    Inorg Chem 46:1315-31. 2007
    ..The bond selectivities of the oxidation of linear and branched alkanes suggest the crucial step in this process to be the attack of a sterically hindered high-valent manganese-oxo species on the C-H bond...
  77. ncbi Cascade reactions using LiAlH4 and grignard reagents in the presence of water
    M Brett Runge
    University of Iowa, Department of Chemistry, Iowa City, IA 52242, USA
    Angew Chem Int Ed Engl 47:935-9. 2008
  78. ncbi Cationic palladium(II)-catalyzed highly enantioselective [3+2] annulation of 2-acylarylboronic acids with substituted alkynes
    Miao Yang
    State Key Laboratory of Organometallic Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Science, 354 Fenglin Road, Shanghai 200032, China
    Org Lett 9:5131-3. 2007
    ..A cationic palladium(II)-catalyzed enantioselective tandem [3+2] annulation of 2-acylarylboronic acids with substituted alkynes to yield optically active 1-indenols was developed in high yields and excellent enantioselectivities...
  79. ncbi An ab initio G3-type/statistical theory study of the formation of indene in combustion flames. II. The pathways originating from reactions of cyclic C5 species-cyclopentadiene and cyclopentadienyl radicals
    V V Kislov
    Department of Chemistry and Biochemistry, Florida International University, Miami, FL 33199, USA
    J Phys Chem A 112:700-16. 2008
    ..The suggested mechanism and computed product yields are consistent with the experimental data obtained in the low-temperature pyrolysis of cyclopentadiene, where indene and naphthalene have been found as the major reaction products...
  80. pmc Two palladium-catalyzed domino reactions from one set of substrates/reagents: efficient synthesis of substituted indenes and cis-stilbenoid hydrocarbons from the same internal alkynes and hindered Grignard reagents
    Cheng Guo Dong
    Department of Chemistry, College of Staten Island and the Graduate Center of the City University of New York, Staten Island, New York 10314, USA
    Org Lett 9:363-6. 2007
    ..Our study provides efficient access to useful polysubstituted indenes and cis-substituted stilbenes and may offer a new means of development of tandem/domino reactions in a more ..
  81. ncbi Michael addition of ortho-lithiated aryloxiranes to alpha,beta-unsaturated malonates: synthesis of tetrahydroindenofuranones
    Antonio Salomone
    Dipartimento Farmaco Chimico, Universita di Bari, Consorzio Interuniversitario Nazionale Metodologie e Processi Innovativi di Sintesi, Via E Orabona 4, I 70125 Bari, Italy
    Org Lett 10:1947-50. 2008
    ..The methodology has been applied to the synthesis of a structural analogue of epipodophyllotoxins...
  82. ncbi Synthesis of indenol- and azulenol derivatives via platinum dichloride-catalyzed intramolecular hydroxy- or alkoxycyclization of cyclic dienynes
    Ming Chang P Yeh
    Department of Chemistry, National Taiwan Normal University, 88 Ding Jou Road, Section 4, Taipei 11677, Taiwan, Republic of China
    J Org Chem 73:2902-4. 2008
    ..4.0.04,8]undecane ring skeleton with extreme diastereoselectivity...
  83. ncbi Efficient synthesis of 3-iodoindenes via Lewis-acid catalyzed Friedel-Crafts cyclization of iodinated allylic alcohols
    Xiaobo Zhou
    Institute of Medicinal Chemistry, Department of Chemistry, East China Normal University, Shanghai, PR China
    J Org Chem 73:3958-60. 2008
    ..Further, the iodoindene derivatives are valuable synthetic building blocks for elaboration of molecular complexity, such as in the construction of multiaryl substituted indenes by Suzuki coupling reaction.
  84. ncbi Indene-based thiazolidinethione chiral auxiliary for propionate and acetate aldol additions
    Antonio Osorio-Lozada
    Division of Medicinal and Natural Products Chemistry, The University of Iowa, Iowa City, Iowa 52242, USA
    Org Lett 10:617-20. 2008
    ..Chlorotitanium enolates of this chiral auxiliary delivered excellent diastereoselectivities in propionate and acetate aldol additions. The chiral auxiliary was easily removed to deliver several valuable functionalities...
  85. ncbi New insight into Ni(II)-catalyzed cyclization reactions of propargylic compounds with soft nucleophiles: novel indenes formation
    Fa Rong Gou
    State Key Laboratory of Applied Organic Chemistry, Lanzhou University, and State Key Laboratory of Solid Lubrication, Lanzhou Institute of Chemical Physics, Chinese Academy of Science, Lanzhou, PR China
    J Org Chem 73:3837-41. 2008
    ..Highly substituted indene derivatives are readily prepared in moderate to excellent yields under very mild reaction conditions in air via a nickel(II)-catalyzed cyclization of propargylic compounds with soft nucleophiles...
  86. ncbi Synthesis of indenes by the palladium-catalyzed carboannulation of internal alkynes
    Daohua Zhang
    Department of Chemistry, Iowa State University, Ames, Iowa 50011, USA
    Org Lett 7:4963-6. 2005
    reaction: see text] A number of highly substituted indenes have been prepared in good yields by treating functionally substituted aryl halides with various internal alkynes in the presence of a palladium catalyst...
  87. ncbi Palladium(0)-catalyzed regioselective and multicomponent synthesis of 1,2,3-trisubstituted 1H-indenes
    Hirokazu Tsukamoto
    Graduate School of Pharmaceutical Sciences, Tohoku University, Aramaki aza aoba 6 3, Sendai 980 8578, Japan
    Org Lett 9:3033-6. 2007
    A multicomponent synthesis of biologically important indenes bearing three substituent groups at the 1-, 2-, and 3-positions from available o-ethynylbenzaldehyde derivatives and organoboron reagents under palladium(0) catalysis is ..
  88. ncbi Synthesis of (-)-sordarin
    Shunsuke Chiba
    Department of Chemistry, Graduate School of Science, The University of Tokyo, 7 3 1 Hongo, Bunkyo ku, Tokyo 113 0033, Japan
    J Am Chem Soc 128:6931-7. 2006
    ....
  89. ncbi An expedited approach to the vitamin D trans-hydrindane building block from the Hajos dione
    Paweł Chochrek
    Institute of Organic Chemistry, Polish Academy of Sciences, ul Kasprzaka 44 52, 01 224 Warsaw 42, Poland
    Org Lett 8:2551-3. 2006
    ..Et(2)O). The diol was selectively deoxygenized either using the Barton-McCombie reaction (with Bu(3)SnH-AIBN) or via the respective iodohydrine (with LiAlH(4)). [reaction: see text]..
  90. ncbi Synthesis, cytotoxicity, DNA interaction, and topoisomerase II inhibition properties of novel indeno[2,1-c]quinolin-7-one and indeno[1,2-c]isoquinolin-5,11-dione derivatives
    Adina Ryckebusch
    UMR 8009 Chimie Organique et Macromoléculaire, Laboratoire de Chimie Organique Physique, Batiment C3 2, Universite des Sciences et Technologies de Lille, 59655 Villeneuve d Ascq, France
    J Med Chem 51:3617-29. 2008
    ..These indeno[1,2- c]isoquinolin-5,11-dione derivatives represent new DNA-topoisomerase II interfering anticancer molecules...
  91. ncbi Metabolism and urinary excretion of a new quinoline anticancer drug, TAS-103, in humans
    R Azuma
    Pharmacokinetics Research Laboratory, Taiho Pharmaceutical Co, Ltd, Tokushima, Japan
    Xenobiotica 32:63-72. 2002
    ..03% of the dose, suggesting that urine is not the main elimination route. TAS-103 was extensively metabolized, and a small percentage of the parent drug (0.41%) was found in urine...
  92. ncbi Discovery of potent poly(ADP-ribose) polymerase-1 inhibitors from the modification of indeno[1,2-c]isoquinolinone
    Prakash G Jagtap
    Inotek Pharmaceuticals Corporation, 100 Cummings Center, Suite 419E, Beverly, MA 01915, USA
    J Med Chem 48:5100-3. 2005
    ..The 9-sulfonamide analogues 11a and 12a exhibited IC(50) values of 1 and 10 nM, respectively...
  93. ncbi Indanoyl amino acid conjugates: tunable elicitors of plant secondary metabolism
    Ryan Lauchli
    Max Planck Institute for Chemical Ecology, D 07745 Jena, Germany
    Chem Rec 3:12-21. 2003
    ..Owing to the strong activation of plant defense or their efficient induction of fruit abscission which facilitates mechanical harvest, the compounds are promising candidates for future application in agriculture...
  94. ncbi Sordarin oxazepine derivatives as potent antifungal agents
    Michael H Serrano-Wu
    Bristol Myers Squibb Pharmaceutical Research Institute, Wallingford, CT 06492, USA
    Bioorg Med Chem Lett 12:2757-60. 2002
    ..The spectrum of antifungal activity for these novel derivatives includes coverage of Candida albicans, Candida glabrata, and Cryptococcus neoformans...
  95. ncbi Antifungal sordarins. Synthesis and structure-activity relationships of 3',4'-fused dioxolane and dioxane derivatives
    José M Bueno
    GlaxoSmithKline, Research Department, Parque Tecnologico de Madrid, Severo Ochoa, 2 28760 Tres Cantos, Madrid, Spain
    Bioorg Med Chem Lett 12:121-4. 2002
    ..A number of novel 3',4'-fused dioxolane and dioxane sordarin derivatives were synthesised for structure-activity relationship studies. Many of these derivatives exhibit high activity against Candida spp. and Cryptococcus neoformans...
  96. ncbi Investigation of substituent effects on the selectivity of 4pi-electrocyclization of 1,3-diarylallylic cations for the formation of highly substituted indenes
    Chris D Smith
    Department of Chemistry, University of Toronto, 80 St George Street, Toronto, Ontario, Canada M5S 3H6
    J Org Chem 75:4716-27. 2010
    ..of a Lewis acid undergo chemoselective and regioselective electrocyclization reactions to generate 1-aryl-1H-indenes. Electrocyclization only occurs for allylic cations bearing a 2-substituent, with 2-ester and 2-alkyl ..
  97. ncbi Unresolved complex mixtures of aromatic hydrocarbons: thousands of overlooked persistent, bioaccumulative, and toxic contaminants in mussels
    Andy M Booth
    Petroleum and Environmental Geochemistry Group, University of Plymouth, Plymouth, PL4 8AA, Devon, U K
    Environ Sci Technol 41:457-64. 2007
    ..of known aromatic hydrocarbons such as branched alkylbenzenes (BABs), tetralins (BATs), and indanes and indenes (BINs)...
  98. pmc Combination of bifunctional alkylating agent and arsenic trioxide synergistically suppresses the growth of drug-resistant tumor cells
    Pei Chih Lee
    Institute of Pharmacology, School of Medicine, National Yang Ming University, Taipei, Taiwan, Republic of China
    Neoplasia 12:376-87. 2010
    ..Our results showed that combining ATO and a synthetic derivative of 3a-aza-cyclopenta[a]indenes (BO-1012), a bifunctional alkylating agent causing DNA interstrand cross-links, was more effective in killing ..
  99. ncbi Evaluation of anti-allergic effects of 1-substituted 2-n-butyl-methylenedioxy indenes
    H Nagai
    Department of Pharmacology, Gifu Pharmaceutical University, Japan
    J Pharmacobiodyn 12:164-9. 1989
    ..The present data indicate the superiority of 1 in both reactions...
  100. ncbi The bioactive conformation of aminoalkylindoles at the cannabinoid CB1 and CB2 receptors: insights gained from (E)- and (Z)-naphthylidene indenes
    P H Reggio
    Department of Chemistry, Kennesaw State University, Kennesaw, Georgia 30144, USA
    J Med Chem 41:5177-87. 1998
    ..Two pairs of (E)- and (Z)-naphthylidene indenes (C-2 H and C-2 Me) were considered...
  101. ncbi Platinum and Ruthenium Chloride-Catalyzed Cycloisomerization of 1-Alkyl-2-ethynylbenzenes: Interception of pi-Activated Alkynes with a Benzylic C-H Bond
    Mamoru Tobisu
    Department of Applied Chemistry, Faculty of Engineering
    J Org Chem 74:5471-5. 2009
    ..and [RuCl(2)(CO)(3)](2), catalyze the cycloisomerization of 1-alkyl-2-ethynylbenzenes to produce substituted indenes even at an ambient temperature...

Research Grants57

  1. Pilot-Scale Heterocyclic and Carbocyclic Libraries for High Throughout Screening
    RICHARD LAROCK; Fiscal Year: 2009
    ..carbolines, isoindolo[2,1-a]indoles, carbazoles, dibenzofurans and various other heterocycles, plus indenones, indenes, fluoren-9-ones and 9-alkylidene-9Hfluorenes...
  2. Synthesis of Medicinally Important Heterocycles
    RICHARD LAROCK; Fiscal Year: 2007
    ..analogues, furans, thiophenes, pyrroles, oxazoles, isoxazoles, pyrazoles, pyridines, quinolines, coumarins, indenes, indenones, naphthols, and phenols...
  3. DAYTIME SLEEPINESS--PREVALENCE, CONSEQUENCES, AND RISKS
    Thomas Roth; Fiscal Year: 2003
    ..The important contribution of the present proposal is that it will be the first population-based study to use laboratory assessments, its consequences and risks to measure sleepiness. ..
  4. PARS inhibitor for cardiac allotransplantation
    Prakash Jagtap; Fiscal Year: 2002
    ..Global markets are estimated at $400 million. Current market entrants such as cyclosporine A and FK506, have substantial toxicity. Funding of SBIR Phases I and II would allow for market entry in 4 years. ..
  5. Novel PARS inhibitor for therapy of colitis
    Prakash Jagtap; Fiscal Year: 2002
    ..These studies will provide the foundation for clinical testing, commercial development, and first market entry of an ultrapotent PARS inhibitor for therapy of IBD. PROPOSED COMMERCIAL APPLICATION: NOT AVAILABLE ..
  6. Novel antioxidant catalyst for transplant rejection
    Prakash Jagtap; Fiscal Year: 2003
    ..Phase II funding would support pharamcokinetic, toxicology, and pharmacodynamic studies required for IND submission and FDA-sanctioned clinical Phase I trials. ..
  7. Novel Single, Dual and Multitargeted Inhibitors of RTKs
    Aleem Gangjee; Fiscal Year: 2007
    ..abstract_text> ..
  8. Light Stimulation of Luteinizing Hormone
    DANIEL KRIPKE; Fiscal Year: 2006
    ..abstract_text> ..
  9. Melatonin Randomized Trial in Insomnia in the Elderly
    Nalaka Gooneratne; Fiscal Year: 2006
    ..abstract_text> ..
  10. b-TrCP E3 Ligase in CLL
    Benjamin Nicholson; Fiscal Year: 2006
    ..unreadable] [unreadable]..
  11. CYP3A Function in Aging AfricanAmericans
    David Greenblatt; Fiscal Year: 2006
    ..This study should provide important mechanistic information on the role of age, gender, and ethnicity as sources of variability in CYP3A-mediated drug metabolism and response. ..
  12. GENETIC VARIANTS IN CIRCADIAN RHYTHM SLEEP DISORDERS
    DANIEL KRIPKE; Fiscal Year: 2006
    ..abstract_text> ..
  13. EFFECT OF GINSENG ON CISPLATIN-INDUCED EMESIS
    Chun Su Yuan; Fiscal Year: 2006
    ..abstract_text> ..
  14. Autonomic dysregulation in primary insomnia
    Gary Richardson; Fiscal Year: 2005
    ..Finally, we will use a new measure of central CRF function, the DEX-sleep latency test, to test the hypothesis that central CRF tone is higher in patients with P1. ..
  15. Synthesis of Cannabinoid Receptor Ligands
    John Huffman; Fiscal Year: 2005
    ..A number of new classical cannabinoids will be synthesized, including additional 1',2'-dimethylheptyl-delta8-tetrahydrocannabinol analogues and the six geminally disubstituted dimethylheptyl-delta8-tetrahydrocannabinols. ..
  16. CARDIOPROTECTIVE EFFECTS OF AMERICAN GINSENG
    Chun Su Yuan; Fiscal Year: 2005
    ..Our results could show that American ginseng extracts have a potential in treating cardiovascular disease. ..
  17. Circadian rhythms and sleep in familial DSPS and ASPS
    Phyllis Zee; Fiscal Year: 2007
    ..abstract_text> ..
  18. Impact of Obesity and Sleep Disorders on Health
    Meir Kryger; Fiscal Year: 2008
    ..This research may show that OSAS is a cause of the high death rate in obesity, making OSAS, not just obesity, a major public health problem. [unreadable] [unreadable] [unreadable]..
  19. Alpha Folate Receptor Mediated GARFTase Inhibitors as Selective Antitumor Agents
    Aleem Gangjee; Fiscal Year: 2010
    ....
  20. Single Agents with Designed Combination Chemotherapy Potential
    Aleem Gangjee; Fiscal Year: 2010
    ..abstract_text> ..
  21. 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. ..
  22. SYNTHESIS OF CANNABINOIDS, ANALOGUES AND METABOLITES
    John Huffman; Fiscal Year: 2009
    ..There a possibility that these metabolites may be contributing to the enhanced potency of cannabinoids with a dimethylheptyl side chain. ..
  23. 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. ..
  24. Genetics, Brain Activity, and Relapse to Alcoholism
    Kirk Brower; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  25. Isopeptide inhibitors for cancer chemotherapy
    Benjamin Nicholson; Fiscal Year: 2008
    ..Compounds that are shown by the assay to inhibit DEN 1 will be evaluated further, and the best of these will be proposed for further development as antitumor agents. [unreadable] [unreadable] [unreadable]..
  26. LIGANDS FOR PROBING THE ACTIVE SITE OF LUMAZINE SYNTHASE
    Mark Cushman; Fiscal Year: 2008
    ..abstract_text> ..
  27. PSYCHOPHARMACOLOGICAL EFFECTS OF EXOGENOUS CHOLINE
    Richard Wurtman; Fiscal Year: 2008
    ..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. Synthesis of New NNRTLs for the Treatment of AIDS
    Mark Cushman; Fiscal Year: 2005
    ..The activities of the ADAMs vs. NNRTI resistant viruses will be investigated. The aqueous solubilities of the new ADAMs will be measured accurately. ..
  30. CHRONIC BENZODIAZEPINES: BEHAVIOR AND NEUROCHEMISTRY
    David Greenblatt; Fiscal Year: 2005
    ....
  31. Third Generation Antiopportunistic Agents
    Aleem Gangjee; Fiscal Year: 2003
    ..Screening against tuberculosis (NIAID) and tumor cells in culture (NCI) is also proposed. ..
  32. NEURAL AND ENDOCRINE REGULATION OF BRAIN AND BEHAVIOR
    Richard Wurtman; Fiscal Year: 2003
    ..abstract_text> ..
  33. Metabolic Consequences of HAART: CYP3A and P-gp
    David Greenblatt; Fiscal Year: 2003
    ..This multidisciplinary proposal provides a clinical and scientific basis to assess the effects of currently available as well as experimental HAART medications on human CYP3A and P-gp. ..
  34. IMPROVING OF CARE BY REVERSAL OF OPIOID CONSTIPATION
    Chun Su Yuan; Fiscal Year: 2003
    ..abstract_text> ..
  35. BEHAVIORAL PHARMACOLOGY OF OPIOIDS
    CHARLES FRANCE; Fiscal Year: 2003
    ....
  36. IMPACT OF SLEEP DISORDERS ON HEALTH
    Meir Kryger; Fiscal Year: 2002
    ....
  37. VERIFICATION OF CIRCADIAN ABNORMALITIES IN AGING
    DANIEL KRIPKE; Fiscal Year: 2002
    ....
  38. STRESS EFFECTS ON SLEEP: INFLUENCE OF GENES AND GENDER
    Fred Turek; Fiscal Year: 2002
    ..abstract_text> ..
  39. PHOTOPERIODIC CONTROL OF REPRODUCTION: EFFECTS OF AGE
    Fred Turek; Fiscal Year: 2001
    ....
  40. HAART Regimens in Substance Abusers
    David Greenblatt; Fiscal Year: 2003
    ....
  41. 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). ..
  42. ROLE OF MELATONIN IN SECONDARY INSOMNIA IN THE ELDERLY
    Nalaka Gooneratne; Fiscal Year: 2004
    ....
  43. Proteomics of M-L antigens modulating cation transport
    PETER LAUF; Fiscal Year: 2004
    ....
  44. ILLUMINATION IN HUMAN AGING: SLEEP AND MOOD EFFECTS
    DANIEL KRIPKE; Fiscal Year: 2004
    ..The success of the treatment in lowering the GDS depression score and in reducing sleep complaints will be examined. ..
  45. RATIONAL PHARMACOTHERAPY OF PRIMARY INSOMNIA
    Daniel Buysse; Fiscal Year: 2004
    ..The Principal Investigator will mentor trainees in analyses of existing data, design and implementation of the clinical trial, described above, and new studies designed by the trainees themselves. ..
  46. Hypoxia-induced apoptosis in a model of sleep apnea
    James McKenna; Fiscal Year: 2004
    ..Overall, it is predicted that the biochemical and apoptotic consequences of IH will be more severe than that of SH, although cellular changes will be observed after both hypoxic exposures. ..
  47. NOVEL NONINDUCIBLE THYMIDYLATE SYNTHASE INHIBITORS
    Aleem Gangjee; Fiscal Year: 2004
    ....
  48. Third Symposium Cell Volume & Signalling Regulation
    PETER LAUF; Fiscal Year: 2003
    ..This meeting's success on U.S. soil will foster continuation of gathering of high-caliber scientists at subsequent international meetings ..
  49. GARLIC PREPARATIONS AND ANTIRETROVIRAL DRUGS
    David Greenblatt; Fiscal Year: 2004
    ..The work will provide immediately applicable clinical data on garlic interactions with antiretrovirals, as well as mechanistic data identifying the interaction process and its predictability from in vitro models. ..
  50. Cardiovascular Effects of Scutellaria baicelensis
    Chun Su Yuan; Fiscal Year: 2002
    ..The results of our project will be used to develop potential new therapeutic agents from active components of Scutellaria baicalensis. ..
  51. PHASE RESPONSE CURVES FOR EXERCISE AND BRIGHT LIGHT
    DANIEL KRIPKE; Fiscal Year: 2002
    ..Resultant circadian phases will then be determined to compute the phase response curves, in order to examine interactions of stimulus (exercise vs. light), age, and gender on circadian responsiveness. ..
  52. GHB abuse: chemistry and neurobiology
    CHARLES FRANCE; Fiscal Year: 2003
    ..abstract_text> ..
  53. BHLH FACTOR IN DIABETES & PANCREAS DEVELOPMENT
    DEBRA BRAMBLETT; Fiscal Year: 2003
    ..The BETA4 knockout will be a mouse model system for the study of aspects of pancreas development and possibly pancreatic disease. ..
  54. ANTIRETROVIRAL THERAPIES AND SUBSTANCE ABUSE
    David Greenblatt; Fiscal Year: 2002
    ..The in vitro model, if validated, has the potential to provide clinically important information on interactions involving HIV treatments and abusable drugs, at relatively low cost and with no human drug exposure. ..
  55. R21 Project: Anti-diabetic Effects of Panax ginseng
    Chun Su Yuan; Fiscal Year: 2003
    ..The results of the proposed project will also help fill gaps in our knowledge before therapeutic agents can be developed. ..
  56. MDR1 and Related Proteins during HIV PI Exposure
    David Greenblatt; Fiscal Year: 2005
    ..The findings will be of importance in understanding lipid disorders related to PIs as well as the kinetics of drugs used to treat HIV and related disorders. ..