Substituted piperidines as HDM2 inhibitors.

Yao Ma, Manami Shizuka,Timothy J Guzi,Yuan Liu,Yuan Tian,Brian R Lahue, Craig R Gibeau,Gerald W Shipps,Yaolin Wang,Stephane Bogen,Latha G Nair,Weidong Pan,Mark Mccoy,Matthew Ernst Voss,Margarita Kirovasnover, Bent W Clayton

Bioorganic & Medicinal Chemistry Letters（2014）

引用 16|浏览38

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摘要

Novel small molecule HDM2 inhibitor, substituted piperidine, was identified. Initial SAR study indicated potential for several position optimizations. Additional potency enhancement was achieved by introducing a sidechain off the aromatic ring. DMPK study of one of the active compounds has shown a moderate oral PK and reasonable bioavailability.

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关键词

HDM2,MDM2,p53,Substituted piperidine,Small molecule inhibitor,Cancer,Oncology

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