pyrones

Summary

Summary: Keto-pyrans.

Top Publications

  1. ncbi Identification and characterization of a novel and specific inhibitor of the ataxia-telangiectasia mutated kinase ATM
    Ian Hickson
    KuDOS Pharmaceuticals Ltd, Cambridge Science Park, Milton Road, Cambridge, UK
    Cancer Res 64:9152-9. 2004
  2. ncbi Pyrones as bacterial signaling molecules
    Alexander O Brachmann
    1 Merck Stiftungsprofessur für Molekulare Biotechnologie, Goethe Universitat Frankfurt, Frankfurt, Germany 2
    Nat Chem Biol 9:573-8. 2013
  3. ncbi From miso, saké and shoyu to cosmetics: a century of science for kojic acid
    Ronald Bentley
    Department of Biological Sciences, University of Pittsburgh, Pittsburgh, PA 15260, USA
    Nat Prod Rep 23:1046-62. 2006
  4. pmc In vitro activity of API-1252, a novel FabI inhibitor, against clinical isolates of Staphylococcus aureus and Staphylococcus epidermidis
    James A Karlowsky
    Antimicrob Agents Chemother 51:1580-1. 2007
  5. ncbi Arzanol, an anti-inflammatory and anti-HIV-1 phloroglucinol alpha-Pyrone from Helichrysum italicum ssp. microphyllum
    Giovanni Appendino
    Dipartimento di Scienze Chimiche, Alimentari, Farmaceutiche e Farmacologiche, Universita del Piemonte Orientale, Via Bovio 6, 28100 Novara, Italy
    J Nat Prod 70:608-12. 2007
  6. ncbi Cytotoxic activity of (S)-goniothalamin and analogues against human cancer cells
    Angelo de Fátima
    Instituto de Quimica, UNICAMP, CP 6154, 13084 971, Campinas, Sao Paulo, Brazil
    Bioorg Med Chem 14:622-31. 2006
  7. ncbi Melasma: a comprehensive update: part II
    Vaneeta M Sheth
    Department of Dermatology at Brigham and Women s Hospital, Harvard Medical School, Boston, Massachusetts, USA
    J Am Acad Dermatol 65:699-714; quiz 715. 2011
  8. ncbi Α-pyrones and diketopiperazine derivatives from the marine-derived actinomycete Nocardiopsis dassonvillei HR10-5
    Peng Fu
    Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, and Affiliated Hospital of Medical College of Qingdao University, Qingdao 266003, People s Republic of China
    J Nat Prod 74:2219-23. 2011
  9. ncbi Identification, cloning, expression, and purification of three novel human calcium-independent phospholipase A2 family members possessing triacylglycerol lipase and acylglycerol transacylase activities
    Christopher M Jenkins
    Division of Bioorganic Chemistry and Molecular Pharmacology, Department of Medicine, Washington University School of Medicine, St Louis, Missouri 63110, USA
    J Biol Chem 279:48968-75. 2004
  10. ncbi Suppression of HIV-1 infection by a small molecule inhibitor of the ATM kinase
    Alan Lau
    KuDOS Pharmaceuticals Limited, 327 Cambridge Science Park, Milton Road, Cambridge CB4 0WG, UK
    Nat Cell Biol 7:493-500. 2005

Detail Information

Publications253 found, 100 shown here

  1. ncbi Identification and characterization of a novel and specific inhibitor of the ataxia-telangiectasia mutated kinase ATM
    Ian Hickson
    KuDOS Pharmaceuticals Ltd, Cambridge Science Park, Milton Road, Cambridge, UK
    Cancer Res 64:9152-9. 2004
    ..We conclude that KU-55933 is a novel, specific, and potent inhibitor of the ATM kinase...
  2. ncbi Pyrones as bacterial signaling molecules
    Alexander O Brachmann
    1 Merck Stiftungsprofessur für Molekulare Biotechnologie, Goethe Universitat Frankfurt, Frankfurt, Germany 2
    Nat Chem Biol 9:573-8. 2013
    ..the insect pathogen Photorhabdus luminescens the orphan LuxR-type receptor PluR detects endogenously produced α-pyrones that serve as signaling molecules at low nanomolar concentrations...
  3. ncbi From miso, saké and shoyu to cosmetics: a century of science for kojic acid
    Ronald Bentley
    Department of Biological Sciences, University of Pittsburgh, Pittsburgh, PA 15260, USA
    Nat Prod Rep 23:1046-62. 2006
    ..It was one of the first secondary metabolites to have its biosynthetic pathway studied by the isotope tracer technique, and, more recently, has been of interest as a skin lightening agent. There are 112 references...
  4. pmc In vitro activity of API-1252, a novel FabI inhibitor, against clinical isolates of Staphylococcus aureus and Staphylococcus epidermidis
    James A Karlowsky
    Antimicrob Agents Chemother 51:1580-1. 2007
  5. ncbi Arzanol, an anti-inflammatory and anti-HIV-1 phloroglucinol alpha-Pyrone from Helichrysum italicum ssp. microphyllum
    Giovanni Appendino
    Dipartimento di Scienze Chimiche, Alimentari, Farmaceutiche e Farmacologiche, Universita del Piemonte Orientale, Via Bovio 6, 28100 Novara, Italy
    J Nat Prod 70:608-12. 2007
    ..Arzanol inhibited HIV-1 replication in T cells and the release of pro-inflammatory cytokines in LPS-stimulated primary monocytes, qualifying as a novel plant-derived anti-inflammatory and antiviral chemotype worth further investigation...
  6. ncbi Cytotoxic activity of (S)-goniothalamin and analogues against human cancer cells
    Angelo de Fátima
    Instituto de Quimica, UNICAMP, CP 6154, 13084 971, Campinas, Sao Paulo, Brazil
    Bioorg Med Chem 14:622-31. 2006
    ..adr)...
  7. ncbi Melasma: a comprehensive update: part II
    Vaneeta M Sheth
    Department of Dermatology at Brigham and Women s Hospital, Harvard Medical School, Boston, Massachusetts, USA
    J Am Acad Dermatol 65:699-714; quiz 715. 2011
    ..A thorough understanding of the risks and benefits of various therapeutic options is crucial in selecting the best treatment...
  8. ncbi Α-pyrones and diketopiperazine derivatives from the marine-derived actinomycete Nocardiopsis dassonvillei HR10-5
    Peng Fu
    Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, and Affiliated Hospital of Medical College of Qingdao University, Qingdao 266003, People s Republic of China
    J Nat Prod 74:2219-23. 2011
    Three new α-pyrones, nocapyrones E-G (1-3), and three new diketopiperazine derivatives, nocazines A-C (4-6), together with a new oxazoline compound, nocazoline A (7), were isolated from the marine-derived actinomycete Nocardiopsis ..
  9. ncbi Identification, cloning, expression, and purification of three novel human calcium-independent phospholipase A2 family members possessing triacylglycerol lipase and acylglycerol transacylase activities
    Christopher M Jenkins
    Division of Bioorganic Chemistry and Molecular Pharmacology, Department of Medicine, Washington University School of Medicine, St Louis, Missouri 63110, USA
    J Biol Chem 279:48968-75. 2004
    ....
  10. ncbi Suppression of HIV-1 infection by a small molecule inhibitor of the ATM kinase
    Alan Lau
    KuDOS Pharmaceuticals Limited, 327 Cambridge Science Park, Milton Road, Cambridge CB4 0WG, UK
    Nat Cell Biol 7:493-500. 2005
    ..Consistent with these observations, we demonstrate that a novel and specific small molecule inhibitor of ATM kinase activity, KU-55933, is capable of suppressing the replication of both wild-type and drug-resistant HIV-1...
  11. ncbi Identification and characterization of a small molecule AMPK activator that treats key components of type 2 diabetes and the metabolic syndrome
    Barbara Cool
    Department of Metabolic Disease Research, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois 60064, USA
    Cell Metab 3:403-16. 2006
    ..These results demonstrate that small molecule-mediated activation of AMPK in vivo is feasible and represents a promising approach for the treatment of type 2 diabetes and the metabolic syndrome...
  12. pmc Mode of action, in vitro activity, and in vivo efficacy of AFN-1252, a selective antistaphylococcal FabI inhibitor
    Nachum Kaplan
    Affinium Pharmaceuticals, Inc, Toronto, ON, Canada
    Antimicrob Agents Chemother 56:5865-74. 2012
    ..These studies, demonstrating a selective mode of action, potent in vitro activity, and in vivo efficacy, support the continued investigation of AFN-1252 as a targeted therapeutic for staphylococcal infections...
  13. pmc Apoptosis of insulin-secreting cells induced by endoplasmic reticulum stress is amplified by overexpression of group VIA calcium-independent phospholipase A2 (iPLA2 beta) and suppressed by inhibition of iPLA2 beta
    Sasanka Ramanadham
    Mass Spectrometry Resource, Division of Endocrinology, Diabetes, and Metabolism, Department of Medicine, Washington University School of Medicine, Box 8127, 660 South Euclid Avenue, St Louis, Missouri 63110, USA
    Biochemistry 43:918-30. 2004
    ..These findings indicate that iPLA(2)beta participates in ER stress-induced apoptosis, a pathway that promotes beta-cell death in diabetes...
  14. pmc Beyond AICA riboside: in search of new specific AMP-activated protein kinase activators
    Bruno Guigas
    Hormone and Metabolic Research Unit, Université catholique de Louvain and de Duve Institute, Brussels, Belgium
    IUBMB Life 61:18-26. 2009
    ..We conclude that A-769662 could be one of the new promising chemical agents to activate AMPK with limited AMPK-independent side effects...
  15. ncbi An assessment of the genotoxicity and human health risk of topical use of kojic acid [5-hydroxy-2-(hydroxymethyl)-4H-pyran-4-one]
    Gerhard J Nohynek
    L Oreal Recherche, Corporate Safety, 25 29, quai Aulagnier, 92600 Asnières, France
    Food Chem Toxicol 42:93-105. 2004
    ..In conclusion, the topical use of KA as a skin lightening agent results in minimal exposure that poses no or negligible risk of genotoxicity or toxicity to the consumer...
  16. ncbi Evaluation of the antioxidant and cytotoxic activity of arzanol, a prenylated alpha-pyrone-phloroglucinol etherodimer from Helichrysum italicum subsp.microphyllum
    Antonella Rosa
    Dipartimento di Biologia Sperimentale, Sez Patologia Sperimentale, Universita degli Studi di Cagliari, Cittadella Universitaria, SS 554, Km 4 5, 09042 Monserrato, Cagliari, Italy
    Chem Biol Interact 165:117-26. 2007
    ..The results of the present work suggest that the natural compound arzanol exerts useful antioxidant properties in different in vitro systems of lipid peroxidation...
  17. ncbi Nocapyrones H-J, 3,6-disubstituted α-pyrones from the marine actinomycete Nocardiopsis sp. KMF-001
    Min Cheol Kim
    Natural Medicine Center, Korea Institute of Science and Technology KIST, Gangneung, Gangwon do 210 340, Republic of Korea
    Chem Pharm Bull (Tokyo) 61:511-5. 2013
    Three new 3,6-disubstituted α-pyrones, nocapyrones H-J (1-3), were isolated from the marine actinomycete Nocardiopsis sp. KMF-001...
  18. ncbi Identity between the Ca2+-independent phospholipase A2 enzymes from P388D1 macrophages and Chinese hamster ovary cells
    M A Balboa
    Department of Chemistry and Biochemistry, University of California at San Diego, La Jolla, California 92093 0601, USA
    J Biol Chem 272:8576-80. 1997
    ..Additionally, covalent modification of the CHO enzyme by [3H]bromoenol lactone is dependent on active enzyme as is the P388D1 iPLA2. Finally, both enzymes have the same specific activities under identical experimental conditions...
  19. pmc A bromoenol lactone suicide substrate inactivates group VIA phospholipase A2 by generating a diffusible bromomethyl keto acid that alkylates cysteine thiols
    Haowei Song
    Medicine Department Mass Spectrometry Facility, Division of Endocrinology, Metabolism, and Lipid Research, Washington University School of Medicine, St Louis, Missouri 63110, USA
    Biochemistry 45:1061-73. 2006
    ....
  20. ncbi Nocapyrones A-D, gamma-pyrones from a Nocardiopsis strain isolated from the marine sponge Halichondria panicea
    Imke Schneemann
    Kieler Wirkstoff Zentrum KiWiZ at the Leibniz Institute of Marine Sciences IFM GEOMAR, Am Kiel Kanal 44, 24106 Kiel, Germany
    J Nat Prod 73:1444-7. 2010
    Four new gamma-pyrones, nocapyrones A-D (1-4), were isolated from an organic extract of the Nocardiopsis strain HB383, which was isolated from the marine sponge Halichondria panicea...
  21. ncbi Arzanol, a prenylated heterodimeric phloroglucinyl pyrone, inhibits eicosanoid biosynthesis and exhibits anti-inflammatory efficacy in vivo
    Julia Bauer
    Department for Pharmaceutical Analytics, Pharmaceutical Institute, University of Tuebingen, Auf der Morgenstelle 8, D 72076 Tuebingen, Germany
    Biochem Pharmacol 81:259-68. 2011
    ..italicum, and a rationale for further pre-clinical evaluation of this novel anti-inflammatory lead...
  22. ncbi The ATM inhibitor KU-55933 suppresses cell proliferation and induces apoptosis by blocking Akt in cancer cells with overactivated Akt
    Yan Li
    Sanford Project and Cancer Biology Research Center, Sanford Research University of South Dakota, Sioux Falls, South Dakota 57104, USA
    Mol Cancer Ther 9:113-25. 2010
    ..Therefore, combining KU-55933 with rapamycin may provide a highly effective approach for improving mammalian target of rapamycin-targeted anticancer therapy that is currently hindered by rapamycin-induced feedback activation of Akt...
  23. ncbi Tyrosine phosphatase inhibition augments collateral blood flow in a rat model of peripheral vascular disease
    Andrew N Carr
    Cardiovascular Research Division, Health Care Research Center, Procter and Gamble Pharmaceuticals, 8700 Mason Montgomery Rd, Box 1064, Mason, OH 45040, USA
    Am J Physiol Heart Circ Physiol 287:H268-76. 2004
    ....
  24. pmc Group VIA phospholipase A2 (iPLA2beta) participates in angiotensin II-induced transcriptional up-regulation of regulator of g-protein signaling-2 in vascular smooth muscle cells
    Zhongwen Xie
    Department of Physiology and the Graduate Center for Nutritional Sciences, University of Kentucky, Lexington, Kentucky 40536, USA
    J Biol Chem 282:25278-89. 2007
    ..Collectively, our results demonstrate that iPLA2beta participates in Ang II-induced transcriptional up-regulation of RGS2 in VSMC...
  25. pmc AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity
    James A Karlowsky
    Department of Medical Microbiology and Infectious Diseases, Faculty of Medicine, University of Manitoba, Winnipeg, Manitoba, Canada
    Antimicrob Agents Chemother 53:3544-8. 2009
    ..Enterobacteriaceae, nonfermentative gram-negative bacilli, and Moraxella catarrhalis. These data support the continued development of AFN-1252 for the treatment of patients with resistant staphylococcal infections...
  26. ncbi Potent, selective pyrone-based inhibitors of stromelysin-1
    David T Puerta
    Department of Chemistry and Biochemistry, Howard Hughes Medical Institute, and Center for Theoretical Biological Physics, University of California San Diego, La Jolla, CA 92093, USA
    J Am Chem Soc 127:14148-9. 2005
    ..The inhibitors demonstrate nanomolar potency against MMP-3 and are selective for MMP-3 over MMP-2 and MMP-1. We postulate that the potency and unusual selectivity profile of these MPI is attributable to the pyrone chelating group...
  27. ncbi Identification of calcium-independent phospholipase A2 (iPLA2) beta, and not iPLA2gamma, as the mediator of arginine vasopressin-induced arachidonic acid release in A-10 smooth muscle cells. Enantioselective mechanism-based discrimination of mammalian iPL
    Christopher M Jenkins
    Division of Bioorganic Chemistry and Molecular Pharmacology, Department of Medicine, Washington University School of Medicine, St Louis, Missouri 63110, USA
    J Biol Chem 277:32807-14. 2002
    ....
  28. pmc Tipranavir-ritonavir genotypic resistance score in protease inhibitor-experienced patients
    Anne Genevieve Marcelin
    Department of Virology, Pitie Salpetriere Hospital, 83 Boulevard de l hopital, 75013 Paris, France
    Antimicrob Agents Chemother 52:3237-43. 2008
    ....
  29. ncbi Citromycetins and bilains A-C: new aromatic polyketides and diketopiperazines from Australian marine-derived and terrestrial Penicillium spp
    Robert J Capon
    Centre for Molecular Biodiversity, Institute for Molecular Bioscience, University of Queensland, St Lucia, Queensland 4072, Australia
    J Nat Prod 70:1746-52. 2007
    ..The citromycin polyketides 2 and 4 and the diketopiperazine 15 were weakly cytotoxic...
  30. ncbi Ca2+-independent phospholipase A2 enhances store-operated Ca2+ entry in dystrophic skeletal muscle fibers
    François Xavier Boittin
    Laboratory of Pharmacology, Geneva Lausanne School of Pharmaceutical Sciences, University of Geneva, University of Lausanne, 1211 Geneva 4, Switzerland
    J Cell Sci 119:3733-42. 2006
    ..The Ca2+-independent phospholipase A2 pathway therefore appears as an attractive target to reduce excessive Ca2+ influx and subsequent degeneration occurring in dystrophic fibers...
  31. ncbi Kojic acid, a secondary metabolite from Aspergillus sp., acts as an inducer of macrophage activation
    Ana Paula D Rodrigues
    Universidade Federal do Par, Instituto de Cincias Biolgicas, Laboratrio de Biologia Estrutural, Belm, Par, Brazil
    Cell Biol Int 35:335-43. 2011
    ..The study demonstrates a new role for KA as a macrophage activator...
  32. pmc Male mice that do not express group VIA phospholipase A2 produce spermatozoa with impaired motility and have greatly reduced fertility
    Shunzhong Bao
    Mass Spectrometry Resource, Division of Endocrinology, Departments of Medicine and of Obstetrics and Gynecology, Washington University School of Medicine, St Louis, Missouri 63110, USA
    J Biol Chem 279:38194-200. 2004
    ....
  33. ncbi Role of an endoplasmic reticulum Ca(2+)-independent phospholipase A(2) in oxidant-induced renal cell death
    Brian S Cummings
    Department of Pharmaceutical Sciences, Medical University of South Carolina, Charleston, South Carolina 29425, USA
    Am J Physiol Renal Physiol 283:F492-8. 2002
    ..These results are the first to demonstrate the expression and subcellular localization of an ER-iPLA(2). These results also suggest that ER-iPLA(2) functions to protect against oxidant-induced lipid peroxidation and oncosis...
  34. ncbi Calcium-independent phospholipase A2 modulates cytosolic oxidant activity and contractile function in murine skeletal muscle cells
    Ming C Gong
    Dept of Physiology, Univ of Kentucky Medical Center, 800 Rose St, Lexington, KY 40536, USA
    J Appl Physiol 100:399-405. 2006
    ..These findings suggest that constitutively expressed iPLA2 modulates oxidant activity in skeletal muscle fibers by supporting ROS production, thereby influencing contractile properties and fatigue characteristics...
  35. ncbi Deoxyverrucosidin, a novel GRP78/BiP down-regulator, produced by Penicillium sp
    Soo Jin Choo
    Laboratory of Antioxidants, Korea Research Institute of Bioscience and Biotechnology, Daejeon 305 333, Korea
    J Antibiot (Tokyo) 58:210-3. 2005
    ..and identified it as a down-regulator of the grp78 gene. The structure of 1 was determined by mainly ESI-mass and two-dimensional NMR spectra. 1 dose-dependently inhibited the expression of GRP78 promoter with an IC50 of 30 nM...
  36. ncbi 2-pyrones possessing antimicrobial and cytotoxic activities
    Ian J S Fairlamb
    Department of Chemistry, University of York, Heslington, York YO10 5DD, UK
    Bioorg Med Chem 12:4285-99. 2004
    ..In an effort to identify synthetic 2-pyrones with interesting biological effects, herein we report the synthesis and biological evaluation of 4-substituted-6-..
  37. pmc Agonist-induced calcium entry correlates with STIM1 translocation
    Kehinde Ross
    Dermatological Sciences, Institute of Cellular Medicine, Medical School, Newcastle University, Newcastle upon Tyne, United Kingdom
    J Cell Physiol 211:569-76. 2007
    ..Thus by differentially regulating store-refilling after agonist-mediated depletion, LPA and UTP may exert distinct effects on the duration of STIM1 localization at the plasma membrane, and thus, on the magnitude and duration of ACE...
  38. ncbi Inhibition of calcium-independent phospholipase A2 activity in rat hippocampus impairs acquisition of short- and long-term memory
    Evelin L Schaeffer
    Laboratory of Neuroscience LIM 27, Department and Institute of Psychiatry, Faculty of Medicine, University of Sao Paulo, Brazil
    Psychopharmacology (Berl) 181:392-400. 2005
    ..In mice, intraperitoneal injections of a selective iPLA(2) inhibitor impaired spatial learning. Accordingly, reduced cPLA(2) and iPLA(2) activities were found in postmortem hippocampus of patients with Alzheimer's disease...
  39. ncbi Polyenylpyrroles and polyenylfurans from an Australian Isolate of the soil ascomycete Gymnoascus reessii
    Benjamin R Clark
    Institute for Molecular Biosciences, University of Queensland, QLD 4072, Australia
    Org Lett 8:701-4. 2006
    ..Structures were assigned with detailed spectroscopic analysis...
  40. ncbi Inhibition of protein tyrosin phosphatase improves vascular endothelial dysfunction
    Dhvanit I Shah
    Department of Pharmaceutical Sciences and Drug Research, Faculty of Medicine, Punjabi University, Patiala 147002 Punjab, India
    Vascul Pharmacol 44:177-82. 2006
    ..Therefore, it may be concluded that BMOV induced inhibition of PTPase may activate eNOS due to opening of ATP sensitive K(+) channels and consequently reduce oxidative stress to improve vascular endothelial dysfunction...
  41. ncbi Cytotoxic flavonoids and alpha-pyrones from Cryptocarya obovata
    Vincent Dumontet
    Institut de Chimie des Substances Naturelles, CNRS, 1, Avenue de la Terrasse, 91198 Gif sur Yvette Cedex, France
    J Nat Prod 67:858-62. 2004
    ..Obolactone (1) and obochalcolactone (3) display significant activity in in vitro cytotoxic assays against the KB cell line. Biosynthetic pathways for oboflavanones and obochalcolactone are suggested...
  42. ncbi 6-[omega-arylalkenyl]-5,6-dihydro-alpha-pyrones from Cryptocarya moschata (Lauraceae)
    A J Cavalheiro
    Instituto de Quimica, Universidade Estadual Paulista, Araraquara, SP, Brazil
    Phytochemistry 53:811-9. 2000
    Eleven 6-[omega-arylalkenyl]-5,6-dihydro-alpha-pyrones, cryptomoscatones D2, E1, E2, E3 and F1 and cryptopyranmoscatones A1, A2, A3, B1, B2 and B4, in addition to goniothalamin and cryptofolione, were isolated from branch and stem bark ..
  43. ncbi In vitro antiproliferative and cytotoxic activities of novel kojic acid derivatives: 5-benzyloxy-2-selenocyanatomethyl- and 5-methoxy-2-selenocyanatomethyl-4-pyranone
    Maria Fickova
    Institute of Experimental Endocrinology, Slovak Academy of Sciences, Vlarska 3, 833 07 Bratislava, Slovak Republic
    J Appl Toxicol 28:554-9. 2008
    ..Cell growth inhibitory activities of new selenium containing kojic acid derivatives are preferentially aimed at the intracellular compartment rather than the plasma membrane and enlarge the group of antiproliferative active compounds...
  44. pmc Solanapyrone analogues from a Hawaiian fungicolous fungus
    Lori E Schmidt
    Department of Chemistry, University of Iowa, Iowa City, Iowa 52242, USA
    J Nat Prod 70:1317-20. 2007
    ..Solanapyrone J (1) showed antifungal activity against Aspergillus flavus and Fusarium verticillioides, while both 1 and 2 showed activity against Staphylococcus aureus and Candida albicans...
  45. ncbi Mixed-ligand copper(II) maltolate complexes: synthesis, characterization, DNA binding and cleavage, and cytotoxicity
    Archika Barve
    Department of Chemistry, University of Pune, Pune 411007, India
    Inorg Chem 48:9120-32. 2009
    ..The cytotoxicity of the complexes against HeLa (cervical) cancer cell lines shows that synergy between the metal and ligands results in a significant enhancement in the cell death with IC(50) of approximately 150-270 microg mL(-1)...
  46. ncbi Oxyresveratrol and hydroxystilbene compounds. Inhibitory effect on tyrosinase and mechanism of action
    Yeon Mi Kim
    College of Pharmacy and Research Center for Bioresource and Health, Chungbuk National University, Cheongju 361 763, Korea
    J Biol Chem 277:16340-4. 2002
    ..The number and position of hydroxy substituents seem to play an important role in the inhibitory effects of hydroxystilbene compounds on tyrosinase activity...
  47. ncbi Synthesis and anticonvulsant activity of new kojic acid derivatives
    Mutlu Dilsiz Aytemir
    Hacettepe University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Ankara, Turkey
    Arzneimittelforschung 60:22-9. 2010
    ....
  48. ncbi Protective role of arzanol against lipid peroxidation in biological systems
    Antonella Rosa
    Dip Biologia Sperimentale, Sez Patologia Sperimentale, Universita degli Studi di Cagliari, Cittadella Universitaria, SS 554, Km 4 5, 09042 Monserrato, Cagliari, Italy
    Chem Phys Lipids 164:24-32. 2011
    ..36×10(-5) and 2.20±0.004×10(-5)cm/s, respectively, suggesting a passive diffusion pathway. The results of the work qualify arzanol as a potent natural antioxidant with a protective effect against lipid oxidation in biological systems...
  49. ncbi Kojic acid-amino acid conjugates as tyrosinase inhibitors
    Jin Mi Noh
    School of Chemical and Biological Engineering, Seoul National University, Seoul 151 744, Republic of Korea
    Bioorg Med Chem Lett 19:5586-9. 2009
    ..It also exhibited dopachrome reducing activity. We also propose a new tyrosinase inhibition mechanism based on the docking simulation data...
  50. ncbi One-pot regio- and stereoselective synthesis of α'-methoxy-γ-pyrones: biological evaluation as mitochondrial respiratory complex inhibitors
    Helena Rosso
    Laboratoire des Fonctions Azotées et Oxygénées Complexes de l IRCOF, CNRS UMR 6014 and FR 3038, Universite de Rouen, Mont Saint Aignan, France
    J Org Chem 76:9429-37. 2011
    The one-pot construction of functionalized α'-methoxy-γ-pyrones is detailed...
  51. ncbi Relative antiviral efficacy of ritonavir-boosted darunavir and ritonavir-boosted tipranavir vs. control protease inhibitor in the POWER and RESIST trials
    A Hill
    Department of Pharmacology, University of Liverpool, Liverpool, UK
    HIV Med 8:259-64. 2007
    ....
  52. ncbi Cytotoxic and antimicrobial metabolites from marine lignicolous fungi, Diaporthe sp
    Xin Lin
    The Key Laboratory of Ministry of Education of Cell Biology and Tumor Engineering, School of Life Science, Xiamen University, Xiamen 361005, PR China
    FEMS Microbiol Lett 251:53-8. 2005
    ..Two known compounds, 7-methoxy-4,6-dimethyl-3H-isobenzofuran-1-one (2) and mycoepoxydiene (3), were also demonstrated to exhibit cytotoxic activities for the first time. All three compounds were assessed for antimicrobial activity...
  53. ncbi Emerging HIV-1 resistance to tipranavir and darunavir in patients with virological failure to first-generation protease inhibitors in Taiwan
    S M Hsieh
    Department of Internal Medicine, National Taiwan University Hospital and National Taiwan UniversityCollege of Medicine, Taipei, Taiwan
    Int J STD AIDS 22:617-20. 2011
    ..Our data revealed a significant increase in the levels of genotypic resistance to TPV and DRV over the past two years in patients with virological failure to first-generation PIs...
  54. ncbi Effects of 3-isobutyl-1-methylxanthine and kojic acid on cocultures and skin equivalents composed of HaCaT cells and human melanocytes
    Marco Springer
    BioTeSys GmbH, Schelztorstrasse 54 56, 73728 Esslingen, Germany
    Arch Dermatol Res 295:88-91. 2003
  55. ncbi Marinactinones A-C, new γ-pyrones from marine actinomycete Marinactinospora thermotolerans SCSIO 00606
    Fazuo Wang
    Key Laboratory of Marine Bio resources Sustainable Utilization, Research Center for Marine Microbes, Guangdong Key Laboratory of Marine Materia Medica, South China Sea Institute of Oceanology, Chinese Academy of Sciences, Guangzhou, PR China
    J Antibiot (Tokyo) 64:189-92. 2011
    Three new γ-pyrones named marinactinones A-C (1-3) were isolated from marine-derived actinomycete Marinactinospora thermotolerans SCSIO 00606. These structures were elucidated by extensive spectroscopic methods...
  56. pmc Efficient synthesis of 5-amido-3-hydroxy-4-pyrones as inhibitors of matrix metalloproteinases
    Yi Long Yan
    Department of Chemistry and Biochemistry, University of California, San Diego, La Jolla, California 92093 0358, USA
    Org Lett 9:2517-20. 2007
    3-hydroxy-4-pyrones are a class of important metal chelators with versatile medicinal applications. An efficient pathway for the preparation of new 5-amido-3-hydroxy-4-pyrone derivatives has been developed...
  57. ncbi Phaeochromycins A-E, anti-inflammatory polyketides isolated from the soil actinomycete Streptomyces phaeochromogenes LL-P018
    Edmund I Graziani
    Department of Chemical and Screening Sciences, Wyeth Research, 401 N Middletown Road, Pearl River, New York 10965, USA
    J Nat Prod 68:1262-5. 2005
    ..Phaeochromycin D (4) is an unusual partially cyclized degraded octaketide intermediate...
  58. ncbi Three dimeric naphtho-γ-pyrones from the mangrove endophytic fungus Aspergillus tubingensis isolated from Pongamia pinnata
    Hong Bo Huang
    School of Chemistry and Chemical Engineering, Sun Yat Sen University, Guangzhou, P R China
    Planta Med 76:1888-91. 2010
    Three new dimeric naphtho-γ-pyrones, named rubasperone A (1), rubasperone B (2), and rubasperone C (3), together with two known compounds, rubrofusarin (4) and rubrofusarin B (5), were isolated from the mangrove endophytic fungus ..
  59. ncbi Bromoenol lactone promotes cell death by a mechanism involving phosphatidate phosphohydrolase-1 rather than calcium-independent phospholipase A2
    Lucia Fuentes
    Institute of Molecular Biology and Genetics, University of Valladolid School of Medicine, E 47005 Valladolid, Spain
    J Biol Chem 278:44683-90. 2003
    ....
  60. ncbi Isolation, Structure elucidation, and antimycobacterial properties of dimeric naphtho-gamma-pyrones from the marine-derived fungus Aspergillus carbonarius
    Yapeng Zhang
    Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, PR China
    Chem Biodivers 5:93-100. 2008
    Two new dimeric naphtho-gamma-pyrones, compounds 1 and 2, were isolated from the AcOEt extract of the fungal strain WZ-4-11 of Aspergillus carbonarius, together with eight known analogues, including 10,10'-bifonsecin B (3), 6'-O-..
  61. ncbi Mycoepoxydiene, a fungal polyketide, induces cell cycle arrest at the G2/M phase and apoptosis in HeLa cells
    Jifeng Wang
    Key Laboratory of the Ministry of Education for Cell Biology and Tumor Cell Engineering, School of Life Sciences, Xiamen University, Xiamen, Fujian, China
    Bioorg Med Chem Lett 20:7054-8. 2010
    ..This study is the first report demonstrating the action mechanism of MED against tumor cell growth. These results provide the potential of MED as a novel low toxic antitumor agent...
  62. ncbi Peritoneal dialysis solutions low in glucose degradation products--evidence for clinical benefits
    Tadashi Tomo
    Faculty of Medicine, Second Department of Internal Medicine, Oita University, Yufu, Japan
    Perit Dial Int 28:S123-7. 2008
    ....
  63. pmc Inhibition of the Rho GTPase, Rac1, decreases estrogen receptor levels and is a novel therapeutic strategy in breast cancer
    ADENA E ROSENBLATT
    Department of Molecular and Cellular Pharmacology, University of Miami Miller School of Medicine, 1600 Northwest 10th Avenue R 189, Miami, Florida 33136, USA
    Endocr Relat Cancer 18:207-19. 2011
    ....
  64. ncbi A nonspecific phosphotyrosine phosphatase inhibitor, bis(maltolato)oxovanadium(IV), improves glucose tolerance and prevents diabetes in Zucker diabetic fatty rats
    Carol L Winter
    Department of Metabolism Biology, Procter and Gamble Pharmaceuticals, 8700 Mason Montgomery Road, Box 1070, Mason, Ohio, 45040
    Exp Biol Med (Maywood) 230:207-16. 2005
    ..These data demonstrate that phosphatase inhibition offers a new approach to diabetes prevention, one that may have advantages over current approaches...
  65. ncbi Virologic and immunologic effectiveness of tipranavir/ritonavir (TPV/r)- versus darunavir/ritonavir (DRV/r)-based regimens in clinical practice
    Tony Antoniou
    University of Toronto, Toronto, Ontario, Canada, Maple Leaf Medical Clinical, Toronto, Ontario, Canada
    J Int Assoc Physicians AIDS Care (Chic) 9:382-9. 2010
    ....
  66. ncbi Food and Drug Administration analysis of tipranavir clinical resistance in HIV-1-infected treatment-experienced patients
    Lisa K Naeger
    Division of Antiviral Products, Center for New Drug Evaluation, Food and Drug Administration, Silver Spring, Maryland, USA
    AIDS 21:179-85. 2007
    ..To assess the resistance profile of tipranavir...
  67. ncbi Regioselective synthesis of kojic acid esters by Bacillus subtilis protease
    Takao Raku
    New Energy and Industrial Technology Development Organization, Tsukuba Central 6, 1 1 1 Higashi, Tsukuba, Ibaraki, 305 8566, Japan
    Biotechnol Lett 25:969-74. 2003
    ..The kojic acid esters had radical scavenging activities, inhibited tyrosinase activity and was biodegradable...
  68. ncbi Antinociceptive properties of coumarins, steroid and dihydrostyryl-2-pyrones from Polygala sabulosa (Polygalaceae) in mice
    Flavia Carla Meotti
    Departamento de Quimica, Universidade Federal de Santa Maria, 97110 000, Santa Maria, RS Brazil
    J Pharm Pharmacol 58:107-12. 2006
    ..The isolated compounds dihydrostyryl-2-pyrones (1, 2, 3), styryl-2-pyrone (7), alpha-spinasterol (9), scopoletin (10) and two esters of the coumarin (scopoletin)..
  69. ncbi Specificity and mechanism of action of EHT 1864, a novel small molecule inhibitor of Rac family small GTPases
    Adam Shutes
    Lineberger Comprehensive Cancer Center, University of North Carolina, Chapel Hill, North Carolina 27599, USA
    J Biol Chem 282:35666-78. 2007
    ..Taken together, our results suggest that EHT 1864 selectively inhibits Rac downstream signaling and transformation by a novel mechanism involving guanine nucleotide displacement...
  70. ncbi Tyrosinase inhibition by extracts and constituents of Sideroxylon inerme L. stem bark, used in South Africa for skin lightening
    S Momtaz
    Department of Plant Science, University of Pretoria, Pretoria 0002, South Africa
    J Ethnopharmacol 119:507-12. 2008
    ..To investigate the stem bark of Sideroxylon inerme L. and its compounds for tyrosinase-inhibition activity and to evaluate the mechanism involved of the most potent compounds in tyrosinase inhibition...
  71. pmc Identification of a small molecule inhibitor of Sir2p
    A Bedalov
    Divisions of Clinical Research, Basic Sciences, and Human Biology, Fred Hutchinson Cancer Research Center, 1100 Fairview Avenue North, Seattle, WA 98109, USA
    Proc Natl Acad Sci U S A 98:15113-8. 2001
    ..By using splitomicin as a chemical genetic probe, we demonstrate that continuous HDA of Sir2p is required for maintaining a silenced state in nondividing cells...
  72. pmc Improved ATM kinase inhibitor KU-60019 radiosensitizes glioma cells, compromises insulin, AKT and ERK prosurvival signaling, and inhibits migration and invasion
    Sarah E Golding
    Department of Radiation Oncology, Virginia Commonwealth University, Richmond, VA 23298 0058, USA
    Mol Cancer Ther 8:2894-902. 2009
    ..Altogether, KU-60019 inhibits the DNA damage response, reduces AKT phosphorylation and prosurvival signaling, inhibits migration and invasion, and effectively radiosensitizes human glioma cells...
  73. pmc Mechanism of action of A-769662, a valuable tool for activation of AMP-activated protein kinase
    Olga Göransson
    Division for Diabetes, Metabolism and Endocrinology, Department of Experimental Medical Science, Lund University, Lund, Sweden
    J Biol Chem 282:32549-60. 2007
    ..We propose that this direct and specific AMPK activator will be a valuable experimental tool to understand the physiological roles of AMPK...
  74. pmc Steady-state disposition of the nonpeptidic protease inhibitor tipranavir when coadministered with ritonavir
    Linzhi Chen
    Departments of Drug Metabolism and Pharmacokinetics, Boehringer Ingelheim Pharmaceuticals, Inc, Ridgefield, Connecticut 06877, USA
    Antimicrob Agents Chemother 51:2436-44. 2007
    ..In conclusion, after the coadministration of TPV and RTV, unchanged TPV represented the primary form of circulating and excreted TPV and the primary extraction route was via the feces...
  75. ncbi 3-O-methylfunicone, a secondary metabolite produced by Penicillium pinophilum, induces growth arrest and apoptosis in HeLa cells
    E Buommino
    Department of Experimental Medicine, Section of Microbiology and Clinical Microbiology, Second University of Naples, Italy
    Cell Prolif 37:413-26. 2004
    ..The capacity of the compound to affect the cell cycle and to modulate apoptosis is indicative of a potential for the development of a new agent for cancer chemotherapy...
  76. ncbi Drug toxicity, HIV progression, or comorbidity of aging: does tipranavir use increase the risk of intracranial hemorrhage?
    Amy C Justice
    Veterans Affairs Connecticut Healthcare System, West Haven, Connecticut 06516, USA
    Clin Infect Dis 47:1226-30. 2008
    ..We studied 2 large cohorts to estimate the background rate of intracranial hemorrhage and compared it with rates reported among persons who had been exposed to tipranavir...
  77. ncbi Detailed reaction mechanism of macrophomate synthase. Extraordinary enzyme catalyzing five-step transformation from 2-pyrones to benzoates
    K Watanabe
    Department of Applied Bioscience, Graduate School of Agriculture, Hokkaido University, Sapporo 060 8589, Japan
    J Biol Chem 275:38393-401. 2000
    ..Incubation of the stereospecifically deuterium-labeled malate with 2-pyrones in the presence of malate dehydrogenase provided information for the stereochemical course of the reaction ..
  78. ncbi Total synthesis of alpha-pyrone meroterpenoids, novel bioactive microbial metabolites
    Toshiaki Sunazuka
    Kitasato Institute for Life Sciences, Kitasato University, and The Kitasato Institute, Shirokane, Minato ku, Japan
    Chem Rev 105:4559-80. 2005
  79. ncbi A role for phospholipase A2 activity in membrane tubule formation and TGN trafficking
    John A Schmidt
    Department of Molecular Biology and Genetics, Cornell University, Ithaca, NY 14853, USA
    Traffic 11:1530-6. 2010
    ..Thus, PLA(2) enzymes appear to have an important role in the earliest steps of membrane tubule formation at the TGN, which are utilized for membrane trafficking...
  80. ncbi Group VIA calcium-independent phospholipase A2 mediates endothelial cell S phase progression
    Shane P Herbert
    Faculty of Biological Sciences, Institute of Molecular and Cellular Biology, University of Leeds, Leeds LS2 9JT, United Kingdom
    J Biol Chem 281:35709-16. 2006
    ..Consequently, iPLA2-VIA is a novel regulator of endothelial cell S phase progression, cell cycle residence, and angiogenesis...
  81. ncbi 2-Pyrone natural products and mimetics: isolation, characterisation and biological activity
    Gerard P McGlacken
    Department of Chemistry, University of York, Heslington, York, UK YO10 5DD
    Nat Prod Rep 22:369-85. 2005
    ..An emphasis has been placed upon the biological activity associated with 2-pyrones, particularly with respect to potential therapeutic or anti-microbial agents...
  82. ncbi Pharmacokinetics, safety, and efficacy of tipranavir boosted with ritonavir alone or in combination with other boosted protease inhibitors as part of optimized combination antiretroviral therapy in highly treatment-experienced patients (BI Study 1182.51)
    Sharon L Walmsley
    Division of Clinical Investigation and Human Physiology, University of Toronto, Toronto, ON, Canada
    J Acquir Immune Defic Syndr 47:429-40. 2008
    ..Given the limited treatment options for patients with high-level resistance, antiretroviral (ARV) regimens based on concomitant use of 2 ritonavir (RTV)-boosted protease inhibitors (PIs) were considered a therapeutic option...
  83. ncbi Methoxy poly(ethylene glycol)-block-poly(delta-valerolactone) copolymer micelles for formulation of hydrophobic drugs
    Helen Lee
    Leslie Dan Faculty of Pharmacy, Department of Pharmaceutical Sciences, and Faculty of Applied Science and Engineering, Division of Engineering Science, University of Toronto, 19 Russell St, Toronto, Ontario, Canada M5S 2S2
    Biomacromolecules 6:3119-28. 2005
    ..The present study indicates that the MePEG-b-PVL copolymers are suitable biomaterials for hydrophobic drug formulation and delivery...
  84. ncbi New beginnings for matrix metalloproteinase inhibitors: identification of high-affinity zinc-binding groups
    David T Puerta
    Department of Chemistry and Biochemistry, University of California, San Diego, La Jolla, California 92093, USA
    J Am Chem Soc 126:8388-9. 2004
    ..These results demonstrate that MPIs based on new ZBGs are feasible and may indeed improve the overall performance of inhibitors designed against these important medicinal targets...
  85. ncbi Significant effects of tipranavir on platelet aggregation and thromboxane B2 formation in vitro and in vivo
    Jochen Graff
    Pharmazentrum Frankfurt, Institute of Clinical Pharmacology at the Johann Wolfgang Goethe University Frankfurt, Germany
    J Antimicrob Chemother 61:394-9. 2008
    ..Recently, the FDA published a warning concerning intracranial haemorrhage in patients taking the HIV-1 protease inhibitor tipranavir co-administered with ritonavir...
  86. ncbi Defining the mechanism of activation of AMP-activated protein kinase by the small molecule A-769662, a member of the thienopyridone family
    Matthew J Sanders
    Cellular Stress Group, Medical Research Council Clinical Sciences Centre, Hammersmith Hospital, Imperial College, DuCane Road, London, United Kingdom
    J Biol Chem 282:32539-48. 2007
    ..Importantly, this model may provide clues for understanding the mechanism by which AMP leads to activation of AMPK, which in turn may help in the identification of other AMPK activators...
  87. ncbi Inhibition of phospholipase A2 reduces neurite outgrowth and neuronal viability
    Orestes V Forlenza
    Laboratory of Neuroscience LIM 27, Department and Institute of Psychiatry, Faculty of Medicine, University of Sao Paulo, Rua Dr Ovidio Pires de Campos s n, 05403 010 Sao Paulo, Brazil
    Prostaglandins Leukot Essent Fatty Acids 76:47-55. 2007
    ..We conclude that the functional integrity of both calcium-dependent and calcium-independent cytosolic PLA2 is necessary for the in vitro development of cortical and hippocampal neurons...
  88. ncbi Tipranavir: a ritonavir-boosted protease inhibitor
    Katherine F Croom
    Adis International Limited, Auckland, New Zealand
    Drugs 65:1669-77; discussion 1678-9. 2005
    ..The most common adverse events in clinical trials of tipranavir were gastrointestinal. The incidence of treatment discontinuation because of adverse events in the RESIST trials was 8% (pooled data)...
  89. ncbi Tipranavir: the first nonpeptidic protease inhibitor for the treatment of protease resistance
    Beatriz Luna
    Wingate University School of Pharmacy, Wingate, North Carolina, USA
    Clin Ther 29:2309-18. 2007
    ..TPV exhibits a resistance profile distinct from that of other currently available PIs, making it a potential option for treatment experienced patients with resistance to multiple Pls...
  90. ncbi Metal complexes of maltol and close analogues in medicinal inorganic chemistry
    Katherine H Thompson
    Medicinal Inorganic Chemistry Group, Chemistry Department, University of British Columbia, Vancouver, BC, Canada V6T 1Z1
    Chem Soc Rev 35:545-56. 2006
    ..The most widely investigated for medicinal applications are the 3-hydroxy-4-pyrones and the 1,2- 3,2- and 3,4-hydroxypyridinones...
  91. ncbi Loss of mitochondrial transmembrane potential and caspase-9 activation during apoptosis induced by the novel styryl-lactone goniothalamin in HL-60 leukemia cells
    S H Inayat-Hussain
    Department of Biomedical Science, Faculty of Allied Health Sciences, Universiti Kebangsaan Malaysia, Jalan Raja Muda Abdul Aziz 50300, Kuala Lumpur, Malaysia
    Toxicol In Vitro 17:433-9. 2003
    ..FMK) abrogated apoptosis as assessed by all of the apoptotic features in this study. In summary, our results demonstrate that goniothalamin-induced apoptosis occurs via the mitochondrial pathway in a caspase dependent manner...
  92. ncbi A novel tricyclic pyrone compound ameliorates cell death associated with intracellular amyloid-beta oligomeric complexes
    Izumi Maezawa
    MIND Institute and Department of Pathology, University of California Davis, Sacramento, California, USA
    J Neurochem 98:57-67. 2006
    ..CP2 analogs represent a new class of promising compounds for the amelioration of Abeta toxicities within both intracellular and extracellular sites...
  93. ncbi Novel tricyclic pyrone compounds prevent intracellular APP C99-induced cell death
    Lee Way Jin
    Department of Pathology, University of Washington, Seattle 98195 7470, USA
    J Mol Neurosci 19:57-61. 2002
    ..Lead compounds will now be selected for their abilities to ameliorate A beta/CTF-mediated pathology in transgenic mice. Our hope is that these compounds may eventually prove beneficial for the prevention and treatment of AD...
  94. ncbi Novel alpha-pyrones produced by a marine Pseudomonas sp. F92S91: taxonomy and biological activities
    Maya P Singh
    Chemical and Screening Sciences, Wyeth Research, Pearl River, NY 10965, USA
    J Antibiot (Tokyo) 56:1033-44. 2003
    ..Culture F92S91, later identified as a Pseudomonas sp. based on 16S profiling, was found to produce two alpha-pyrones (I and II) and three high molecular weight peptides...
  95. ncbi Goniothalamin induces apoptosis in vascular smooth muscle cells
    K M Chan
    Department of Biomedical Science, Faculty of Allied Health Sciences, Universiti Kebangsaan Malaysia, Jalan Raja Muda Abdul Aziz, 50300 Kuala Lumpur, Malaysia
    Chem Biol Interact 159:129-40. 2006
    ..Moreover, GN effects were comparable to rapamycin. In conclusion, our data show that GN initially induces DNA damage which subsequently leads to cytotoxicity primarily via apoptosis in VSMCs...
  96. ncbi The clinical development of new mitotic inhibitors that stabilize the microtubule
    Sridhar Mani
    Departments of Medicine and Oncology, Albert Einstein College of Medicine, Montefiore and Jacobi Medical Center, Bronx, NY, USA
    Anticancer Drugs 15:553-8. 2004
    ..There is now considerable data regarding the efficacy of the epothilones in human beings and discodermolide holds such promise, as well...
  97. ncbi The structure activity relationship of discodermolide analogues
    Simon J Shaw
    Kosan Biosciences, Inc 3832 Bay Center Place, Hayward, CA 94545, USA
    Mini Rev Med Chem 8:276-84. 2008
    ..The majority of analogues have been generated via modification of the lactone region. This suggests that significant simplifications can be made in this region provided that the lactone moiety is maintained...
  98. ncbi Goniothalamin induces cell cycle-specific apoptosis by modulating the redox status in MDA-MB-231 cells
    Wen Ying Chen
    Graduate Institute of Natural Products, Kaohsiung Medical University, Kaohsiung City, Taiwan
    Eur J Pharmacol 522:20-9. 2005
    ....
  99. ncbi Synergistic suppression of microtubule dynamics by discodermolide and paclitaxel in non-small cell lung carcinoma cells
    Stephane Honore
    FRE CNRS 2737, Universite de la Mediterranee, Marseille, France
    Cancer Res 64:4957-64. 2004
    ....
  100. ncbi Enantioselective synthesis of apoptolidinone: exploiting the versatility of thiazolidinethione chiral auxiliaries
    Michael T Crimmins
    Department of Chemistry, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599 3290, USA
    J Am Chem Soc 127:13810-2. 2005
    ..A cross-metathesis reaction is utilized to assemble the C1-C10 trieneoate fragment and the C11-C28 polypropionate region of the molecule...
  101. ncbi Ca2+-independent phospholipase A2 is a novel determinant of store-operated Ca2+ entry
    Tarik Smani
    Boston University School of Medicine, Boston, Massachusetts 02118, USA
    J Biol Chem 278:11909-15. 2003
    ..Thus, functional iPLA(2) is required for activation of store-operated channels and capacitative Ca(2+) influx in wide variety of cell types...

Research Grants62

  1. Pilot-Scale Heterocyclic and Carbocyclic Libraries for High Throughout Screening
    RICHARD LAROCK; Fiscal Year: 2009
    ..to prepare specially diverse libraries of indoles, benzofurans, benzopyrans, coumarins, isocoumarins, phthalides, pyrones, 2-quinolones, pyridines, isoquinolin-1-ones, isoindolin-1-ones, isoquinolines, carbolines, isoindolo[2,1-a]..
  2. Structural Facets of the Inhibition of Alzheimer's Amyloid-beta Oligomers by Tric
    Nathan A Oyler; Fiscal Year: 2012
    ..A class of small organic compounds has been discovered, namely tricyclic pyrones (TP), such as CP2 (code name), that prevents the death of human neuroblastoma MC65 cells related to intracellular ..
  3. ASYMMETRIC SYNTHESIS OF PHYSIOLOGICALLY ACTIVE COMPOUNDS
    Gary Posner; Fiscal Year: 1992
    ..understanding of asymmetric inverse-electron-demand Diels-Alder cycloadditions between electron-deficient pyrones and pyridones and electron-rich dienophiles...
  4. Total Synthesis of Biologically Active Gamma-Pyrones
    Dirk Trauner; Fiscal Year: 2007
    ..In a further contribution to synthetic methodology, new approaches towards gamma-pyrones are proposed...
  5. Transition Metal Mediated Routes to Heterocycles and Carbocycles
    Janis Louie; Fiscal Year: 2009
    ..involving nickel-based catalysts for mediating carbon dioxide/diyne and isocyanate/diyne annulations to produce 2-pyrones and 2-pyridones, respectively...
  6. Inhibition of Alzheimer's Beta-Amyloid Fibril Formation
    Duy Hua; Fiscal Year: 2009
    ..In search of a compound that blocks this conformational change, we discovered that a class of tricyclic pyrones (TP), especially CP2 (code name), prevents the death of human neuroblastoma MC65 cells related to intracellular ..
  7. SYNTHESIS OF SPONGISTATIN ANTITUMOR AGENTS
    AMOS SMITH; Fiscal Year: 2007
    ..abstract_text> ..
  8. NMR systems : 2 Bruker Avance 500 Consoles
    AMOS SMITH; Fiscal Year: 2006
    ..The areas of public health research include, among others, cancer, infectious diseases, neurodegenerative diseases such as Alzheimer's disease, and heart and cardiovascular disease. [unreadable] [unreadable] [unreadable]..
  9. SYNTHESIS OF CHLOROPEPTINS, GP120 CD4 BINDING INHIBITORS
    AMOS SMITH; Fiscal Year: 2001
    ..abstract_text> ..
  10. Design and Synthesis of HIV-1 Protease Inhibitors
    AMOS SMITH; Fiscal Year: 2004
    ....
  11. 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. ..
  12. Natural Product Leads for Drug Development
    KATHLYN PARKER; Fiscal Year: 2009
    ..Molecular modeling will allow the design of candidates for more active drugs. Candidates will be evaluated in the squalene synthase assay. Collaborations for the medicinal chemistry components of the project have been arranged. ..
  13. STRATEGIES AND METHODS IN SYNTHESIS OF NATURAL PRODUCTS
    KATHLYN PARKER; Fiscal Year: 2003
    ..During the period which corresponds to this proposal, we plan to apply our new methodology to the synthesis of deacetylravidomycin and kidamycin, representatives of the remaining two major classes. ..
  14. 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. ..
  15. 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. ..
  16. 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. ..
  17. Novel antibacterial agents for treatment of Tularemia
    Nachum Kaplan; Fiscal Year: 2004
    ..tularensis microbiological data and animal model data to warrant inclusion of the information on the product label as a narrow spectrum agent that could be used in the event of a F. tularensis release. ..
  18. 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. ..
  19. 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. ..
  20. Understanding and Altering the Virologic Setpoint
    Martin Markowitz; Fiscal Year: 2006
    ..abstract_text> ..
  21. Cellular Targets for Gallium Compounds in Lymphoma
    Christopher Chitambar; Fiscal Year: 2008
    ..Our studies will provide new information regarding: a) the impact of HFE mutations on the response of lymphoma to gallium, and, b) the mechanism of action of gallium at the mitochondrial level. ..
  22. FLUOROUS METHODS FOR TRADITIONAL AND PARALLEL SYNTHESIS
    DENNIS CURRAN; Fiscal Year: 2003
    ..In short, the work will help to move the very young field of fluorous chemistry from infancy into childhood. ..
  23. Purchase of a 600 MHz NMR Spectrometer with Cryoprobe
    DENNIS CURRAN; Fiscal Year: 2007
    ..This research often requires sophisticated NMR experiments on small samples, and the requested 600 MHz spectrometer will greatly expedite ongoing and planned work. [unreadable] [unreadable] [unreadable]..
  24. Molecular Target Focused Discovery of Anticancer Drugs
    GEORGE PETTIT; Fiscal Year: 2007
    ..In summary, the proposed research will be sharply aimed at the discovery and very rapid development of new anticancer drugs for the NCI programs direct at improving human cancer treatments. ..
  25. Molecular Target Focused Discovery of Anticancer Drugs
    George R Pettit; Fiscal Year: 2010
    ....
  26. RADICAL REACTIONS FOR NATURAL PRODUCTS
    DENNIS CURRAN; Fiscal Year: 2002
    ....
  27. The Transmission and Fitness of Drug Resistant HIV-1
    MARTIN H MARKOWITZ; Fiscal Year: 2011
    ..abstract_text> ..
  28. Host Polymorphisms and Uncomplicated Malaria
    Sunil Parikh; Fiscal Year: 2008
    ..Parikh will be able to utilize modern molecular epidemiology techniques to investigate human genetic factors underlying susceptibility to malaria and he will be well equipped for a career in academic research. ..
  29. STRATEGIES FOR CONTEXT SPECIFIC ANTICANCER THERAPIES
    Julian Simon; Fiscal Year: 2002
    ..Together, the studies outlined in our Specific Aims, will constitute the first step in testing the hypothesis of context-specific toxicity in cancer chemotherapy. ..
  30. SYNTHESIS OF NOVEL BIOLOGICALLY ACTIVE NATURAL PRODUCTS
    ROBERT BOECKMAN; Fiscal Year: 2002
    ..The hypothesis that an internal chelate of suitably disposed oxygen functions permits the modification of the ring conformation from half-chair to half-boat will be tested. ..
  31. Azinomycins - Total Synthesis and Mechanism of Action
    Robert Coleman; Fiscal Year: 2007
    ..abstract_text> ..
  32. Midcareer Investigator Award /Patient-Oriented Research
    Charles Hicks; Fiscal Year: 2008
    ..unreadable] [unreadable]..
  33. Epothilone Analogs by Partial Chemical Synthesis
    David Myles; Fiscal Year: 2002
    ..The proposed epothilone analogs with increased solubility will have a potentially competitive advantage for a $2 billion per year market for the treatment of breast, lung and ovarian cancers. ..
  34. NOVEL DOUBLE STRAND BREAK PRODUCING COMPOUNDS
    Julian Simon; Fiscal Year: 2001
    ..The yeast experiments will involve both classical genetic approaches and genome-wide analyses based on DNA microarray technology. ..
  35. Theory of the Chemistry of NO, HNO, OONO-, and RSNO
    KENDALL HOUK; Fiscal Year: 2009
    ..The success of the research described here can lead to new tools for study of physiological processes and drugs for hypertension, cardiac failure, and other biological processes involving NO metabolism. ..
  36. Synthetic Reactions Catalyzed by Transition Metals
    Ei ichi Negishi; Fiscal Year: 2010
    ..Being considered for this purpose are discodermolide, hennoxazole A, zincophorin, roselipins, apoptolidin, nafuredin, caIlystatin A, milbemycin p3, calyculin A, and amphotericin B. ..
  37. Biosynthesis of Hypotensive Phosphonopeptide Natural Products
    Brian O Bachmann; Fiscal Year: 2010
    ..Metalloproteinase inhibitors have potential to treat a large number of human illnesses including hypertension, cancer and osteoarthritis, among others. ..
  38. CHEMICAL SYNTHESIS OF NOVEL NATURAL PRODUCTS
    David Williams; Fiscal Year: 2009
    ..Daphnicyclidin A. This recent discovery has revealed a new molecular architecture which exhibits significant antitumor activity. Our research will investigate strategies for chemical synthesis of these complex polycyclic systems. ..
  39. Inhibitors of Hedgehog Signaling For Brain Cancer Chemotherapy
    JEFFREY D contact WINKLER; Fiscal Year: 2010
    ..The studies outlined herein therefore hold the promise of developing important new tools in cancer biology and new drug candidates for the treatment of brain cancers. ..
  40. Regulation of vascular smooth muscle calcium sensitivity
    Paul H Ratz; Fiscal Year: 2010
    ..The Specific Aim of this study will be to test the hypothesis that ROK and PKCzeta both mediate KCI- induced Ca sensitization of FA, and that iPLA2 and PI3K are required as upstream activators of ROK and PKCzeta. ..
  41. Novel Ribostamycins and SAR Study of Ring III Aminosugar
    Cheng Wei Chang; Fiscal Year: 2008
    ..unreadable] [unreadable]..
  42. Induction of Autophagy in Human Macrophages by Lipopolysaccharide
    Beatrice Haimovich; Fiscal Year: 2008
    ..To determine whether LPS-induced mitochondrial dysfunction results in HMDM autophagy. Aim 2. To determine whether autophagy enhances the resistance of LPS-treated HMDM to Gram-negative bacteria. ..
  43. Immunity in Early Syphillis: Pathway to HIV Coinfection
    Juan Salazar; Fiscal Year: 2007
    ..In Aim 2 we will study the effect of secondary syphilis on viral load (VL) in HIV co-infected individuals. In this aim we will compare VL between HIV patients with and without syphilis and determine the effect of penicillin on VL. ..
  44. Nociception in Diabetic Neuropathy: Role of Endothelins
    Liliana Berti Mattera; Fiscal Year: 2004
    ..abstract_text> ..
  45. BASIS FOR ALCOHOL AND COCAINE STROKES--ROLE OF MG2+
    Burton Altura; Fiscal Year: 2004
    ..An understanding of how ethanol and cocaine induce strokes may ultimately suggest new targets for pharmacologic manipulation, and thus, improving the clinical outcome after "binge- drinking" or cocaine intoxication. ..
  46. Efficient synthesis of discodermolide
    Gary Ashley; Fiscal Year: 2005
    ..abstract_text> ..
  47. CaBP4, a Photoreceptor Specific Calcium-Binding Protein
    Francoise Haeseleer; Fiscal Year: 2005
    ..The mechanism of interaction of CaBP4 with its target will also be examined using both in vitro and in vivo procedures. ..
  48. NEW DEVELOPMENTS IN ORGANOCOPPER CHEMISTRY
    R Dieter; Fiscal Year: 2004
    ..The proposed synthetic routes to pyrrolidine aza sugars will develop the potential synthetic power of alpha-aminoalkylcuprate chemistry. ..
  49. MECHANISM OF PLATELET ACTIVATION ON MATRIX PROTEINS
    Beatrice Haimovich; Fiscal Year: 2004
    ..phosphatase(s) and kinase(s) regulate the state of phosphorylation of a-actinin? Aim 3: What is the role of tyrosine phosphorylation of pplOl and vinculin, and which phosphatase(s) and kinase(s) regulate these phosphorylation events? ..
  50. New mitosis specific anticancer agents
    Julian Simon; Fiscal Year: 2005
    ..Through these convergent studies we hope to identify new mitosis-specific anticancer agents, their targets and the contexts in which these compounds are most effective. ..
  51. SYNTHETIC STUDIES RELATED TO CANCER RESEARCH/TREATMENT
    Paul Wender; Fiscal Year: 2005
    ..Overall, this research program is expected to be of significant value in chemistry, biology, and medicine. ..
  52. Irreversible inhibitors of cholesterol esterase
    LORRAINE DECK; Fiscal Year: 2005
    ....
  53. Apoptosis and transport mechanisms in neurodegeneration
    David DeWitt; Fiscal Year: 2002
    ..Cytoskeletal abnormalities including tau phosphorylation, neurofilament accumulation, and microtubule disruption will be examined to determine whether these changes. ..
  54. Motilin Receptor Agonists for Diabetic Gastroperesis
    David Myles; Fiscal Year: 2005
    ....
  55. Asymmetric Synthesis of Cytotoxic Natural Products
    Robert Coleman; Fiscal Year: 2005
    ..abstract_text> ..
  56. INTERESTING BIOACTIVE SUBSTANCES
    David Williams; Fiscal Year: 2006
    ..The selective synthesis of contiguous stereotriads will advance basic methodology for asymmetric conjugate additions. ..
  57. ANTIRETROVIRAL PHARMACOLOGY IN THE GENITAL TRACT
    Angela Kashuba; Fiscal Year: 2007
    ..abstract_text> ..
  58. Vinylogous Amide Photochemistry in Organic Synthesis
    Jeffrey Winkler; Fiscal Year: 2005
    ..abstract_text> ..
  59. REGULATION OF DETRUSOR SMOOTH MUSCLE CONTRACTION
    PAUL RATZ; Fiscal Year: 2005
    ..Collectively, these studies will provide new insights into the cellular mechanisms regulating DSM contractions. ..
  60. ACYCLIC STEREOCONTROL IN RADICAL REACTIONS
    MUKUND SIBI; Fiscal Year: 2007
    ..3. The conversion of readily available pyrones to chiral pyran building blocks, a common skeleton found in marine natural products with potent biological ..
  61. SYNTHESIS OF THE TEDANOLIDES, CYTOTOXIC POLYPROPIONATES
    Michael Jung; Fiscal Year: 2003
    ....