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

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• 作者：Yuan Tian^a ; ^{yuan.tian2@merck.com" class="auth_mail" title="E-mail the corresponding author} ; Yao Ma^a ; Craig R. Gibeau^a ; Brian R. Lahue^a ; Gerald W. Shipps Jr.^a ; Corey Strickland^b ; Sté ; phane L. Bogen^b
• 关键词：p53 ; hDM2 ; SAR
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：1 June 2016
• 年：2016
• 卷：26
• 期：11
• 页码：2735-2738
• 全文大小：2296 K

文摘

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.