- Discovery and Evaluation of BMS-708163, a Potent, Selective and Orally Bioavailable gamma-Secretase Inhibitor
[作者:GILLMAN KEVIN W; STARRETT JOHN E JR; PARKER MICHAEL F; XIE KAI; BRONSON JOANNE J; MARCIN LAWRENCE R; MCELHONE KATE E; BERGSTROM CARL P; MATE ROBERT A; WILLIAMS RICHARD; MEREDITH JERE E JR; BURTON CATHERINE R; BARTEN DONNA M; TOYN JEREMY H; ROBERTS SUSAN B; LENTZ KIMBERLEY A; HOUSTON JOHN G; ZACZEK ROBERT; ALBRIGHT CHARLES F; DECICCO CARL P; MACOR JOHN E; OLSON RICHARD E,期刊:ACS Medicinal Chemistry Letters, 页码:120-124 , 文章类型: Article,,卷期:2010年1-3]
- During the course of our research efforts to develop a potent and selective gamma-secretase inhibitor for the treatment of Alzheimer's disease, we investigated a series of carboxamide-substituted sulfonamides. Optimizati...
- Discovery of NVP-LDE225, a Potent and Selective Smoothened Antagonist
[作者:PAN SHIFENG; WU XU; JIANG JIQING; GAO WENQI; WAN YONGQIN; CHENG DAI; HAN DONG; LIU JUN; ENGLUND NATHAN P; WANG YAN; PEUKERT STEFAN; MILLERMOSLIN KAREN; YUAN JING; GUO RIBO; MATSUMOTO MELISSA; VATTAY ANTHONY; JIANG YUN; TSAO JEFFREY; SUN FANGXIAN; PFERDEKAMPER ANNEMARIE C; DODD STEPHANIE; TUNTLAND TOVE; MANIARA WIESLAWA; KELLEHER JOSEPH F III; YAO YUNGMAE; WARMUTH MARKUS; WILLIAMS JULIET; DORSCH MARION,期刊:ACS Medicinal Chemistry Letters, 页码:130-134 , 文章类型: Article,,卷期:2010年1-3]
- The blockade of aberrant hedgehog (Hh) signaling has shown promise for therapeutic intervention in cancer. A cell-based phenotypic high-throughput screen was performed, and the lead structure (1) was identified as an inh...
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