Discovery of a highly potent CECR2 bromodomain inhibitor with 7H-pyrrolo[2,3-d] pyrimidine scaffold

Haibo Lu,Tian Lu,Shijia Zu,Zhe Duan,Yiman Guang,Qi Li,Jingyi Ma,Dongying Chen,Bo Li,Wenchao Lu,Hualiang Jiang,Cheng Luo,Deyong Ye,Kaixian Chen,Hua Lin

Bioorganic Chemistry（2022）

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摘要

•The binding models of TP-248 with CECR2 BRD and BPTF BRD were analyzed.•Intensive SAR study lead to a highly potent compound DC-CBi-22.•DC-CBi-22 with high potency and selectivity was obtained.•The SARs were explained based on molecular docking.•The binding of DC-CBi-22 to CECR2-BRD was verified by biochemical and physiological methods.

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关键词

CECR2 bromodomain,BPTF bromodomain,Small-molecule inhibitor,SAR study,Chemical probe

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