Design, synthesis and biological evaluation of 2-aminopyridine derivatives as USP7 inhibitors

Xiaoming Xu, Mingchen Wang, Hailong Xu,Na Liu,Kaixian Chen,Cheng Luo,Shijie Chen,Hua Chen

Bioorganic Chemistry（2022）

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摘要

•Novel 2-aminopyridine derivatives have been rationally designed and conveniently synthesized.•Compound 7 inhibited USP7 markedly with IC50 value of 7.6 μM.•Compounds 7 and 21 expressed significant binding interactions with USP7 by SPR-based binding assay.•Compounds 7 and 21 could effectively promote MDM2 degradation, p53 stabilization and p21 gene expression.

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关键词

Aminopyridine,USP7 inhibitors,Suzuki coupling reaction,Colorectal carcinoma,MDM2,P53 and p21

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