Functionalized N,N-Diphenylamines as Potent and Selective EPAC2 Inhibitors

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• 作者：Christopher T. Wild ; Yingmin Zhu ; Ye Na ; Fang Mei ; Marcus A. Ynalvez ; Haiying Chen ; Xiaodong Cheng ; Jia Zhou
• 刊名：ACS Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：May 12, 2016
• 年：2016
• 卷：7
• 期：5
• 页码：460-464
• 全文大小：388K
• 年卷期：0
• ISSN：1948-5875

文摘

N,N-Diphenylamines were discovered as potent and selective EPAC2 inhibitors. A study was conducted to determine the structure–activity relationships in a series of inhibitors of which several compounds displayed submicromolar potencies. Selectivity over the related EPAC1 protein was also demonstrated. Computational modeling reveals an allosteric site that is distinct from the cAMP binding domain shared by both EPAC isoforms, providing a theory with regards to subtype selectivity.