Structure-activity relationship study of 4-substituted piperidines at Leu26 moiety of novel p53-hDM2 inhibitors.

Yuan Tian,Yao Ma,Craig R Gibeau,Brian R Lahue,Gerald W Shipps,Corey Strickland,Stéphane L Bogen

Bioorganic & Medicinal Chemistry Letters（2016）

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摘要

Led by the structural information of the screening hit with mDM2 protein, a structure modification of Leu26 moiety of the novel p53–hDM2 inhibitors was conducted. A structure–activity relationship study of 4-substituted piperidines revealed compound 20t with good potencies and excellent CYP450 profiles.

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p53,hDM2,SAR

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