- Novel Steroid Inhibitors of Glucose 6-Phosphate Dehydrogenase
[作者:HAMILTON NIALL M; DAWSON MARTIN; FAIRWEATHER EMMA E; HAMILTON NICOLA S; HITCHIN JAMES R; JAMES DOMINIC I; JONES STUART D; JORDAN ALLAN M; LYONS AMANDA J; SMALL HELEN F; THOMSON GRAEME J; WADDELL IAN D; OGILVIE DONALD J,期刊:Journal of Medicinal Chemistry, 页码:4431-4445 , 文章类型: Article,,卷期:2012年55-9]
- Novel derivatives of the steroid DHEA 1, a known uncompetitive inhibitor of G6PD, were designed, synthesized, and tested for their ability to inhibit this dehydrogenase enzyme. Several compounds with approximately 10-fol...
- Methyl Effects on Protein-Ligand Binding
[作者:LEUNG CHERYL S; LEUNG SIEGFRIED S F; TIRADORIVES JULIAN; JORGENSEN WILLIAM L,期刊:Journal of Medicinal Chemistry, 页码:4489-4500 , 文章类型: Article,,卷期:2012年55-9]
- The effects of addition of a methyl group to a lead compound on biological activity are examined. A literature analysis of > 2000 cases reveals that an activity boost of a factor of 10 or more is found with an 8% frequen...
- Discovery of a Potent Small-Molecule Antagonist of Inhibitor of Apoptosis (IAP) Proteins and Clinical Candidate for the Treatment of Cancer (GDC-0152)
[作者:FLYGARE JOHN A; BERESINI MAUREEN; BUDHA NAGESHWAR; CHAN HELEN; CHAN IRIS T; CHEETI SRAVANTHI; COHEN FREDERICK; DESHAYES KURT; DOERNER KARL; ECKHARDT S GAIL; ELLIOTT LINDA O; FENG BAINIAN; FRANKLIN MATTHEW C; REISNER STACY FRANKOVITZ; GAZZARD LEWIS; HALLADAY JASON; HYMOWITZ SARAH G; LA HANK; LORUSSO PATRICIA; MAURER BRIGITTE; MURRAY LESLEY; PLISE EMILE; QUAN CLIFFORD; STEPHAN JEANPHILIPPE; YOUNG SHIN G; TOM JEFFREY; TSUI VICKIE; UM JOANNE; VARFOLOMEEV EUGENE; VUCIC DOMAGOJ; WAGNER ANDREW J; WALLWEBER HEIDI J A; WANG LAN; WARE JOSEPH; WEN ZHAOYANG; WONG HARVEY; WONG JONATHAN M; WONG MELISA; WONG SUSAN; YU RON; ZOBEL KERRY; FAIRBROTHER WAYNE J,期刊:Journal of Medicinal Chemistry, 页码:4101-4113 , 文章类型: Article,,卷期:2012年55-9]
- A series of compounds were designed and synthesized as antagonists of cIAP1/2, ML-IAP, and XIAP based on the N-terminus, AVPI, of mature Smac. Compound 1 (GDC-0152) has the best profile of these compounds; it binds to th...
- Discovery of Novel 1,2,4-Thiadiazole Derivatives as Potent, Orally Active Agonists of Sphingosine 1-Phosphate Receptor Subtype 1 (S1P(1))
[作者:REN FENG; DENG GUANGHUI; WANG HAILONG; LUAN LINBO; MENG QINGHUA; XU QIONGFENG; XU HENG; XU XUESONG; ZHANG HAIBO; ZHAO BAOWEI; LI CHENGYONG; GUO TAYLOR B; YANG JIANSONG; ZHANG WEI; ZHAO YONGGANG; JIA QIANTAO; LU HONGTAO; XIANG JIANING; ELLIOTT JOHN D; LIN XICHEN,期刊:Journal of Medicinal Chemistry, 页码:4286-4296 , 文章类型: Article,,卷期:2012年55-9]
- A novel series of 1,2,4-thiadiazole compounds was discovered as selective S1P(1) agonists. The extensive structure-activity relationship studies for these analogues were reported. Among them, 17g was identified to show h...
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