Discovery and structural insight of a highly selective protein kinase inhibitor hit through click chemistry

Guoxian Gu; Huihui Wang; Pi Liu; Chenzeng Fu; Zhonghua Li; Xuefeng Cao; Yunping Li; Qinghong Fang; Feng Xu; Jie Shen; Peng George Wang

doi:10.1039/C1CC15851A

Discovery and structural insight of a highly selective protein kinase inhibitor hit through click chemistry†

Guoxian Gu,‡^a Huihui Wang,‡^a Pi Liu,‡^a Chenzeng Fu,^a Zhonghua Li,^a Xuefeng Cao,^a Yunping Li,^a Qinghong Fang,^a Feng Xu,^a Jie Shen*^a and Peng George Wang*^a

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^a College of Pharmacy and Tianjin Key Laboratory of Molecular Research, State Key Laboratory of Medicinal Chemical Biology, Nankai University, Tianjin, P. R. China
E-mail: jieshen@nankai.edu.cn

Abstract

Novel bisaryl maleimide derivatives to mimic natural kinase inhibitors were prepared through click chemistry. A highly selective hit was discovered in a 124-kinase-assay, and docking studies revealed a π–π stacking interaction with the Phe67 at the P-loop of GSK-3β kinase.

Chemical Communications

Discovery and structural insight of a highly selective protein kinase inhibitor hit through click chemistry†

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Discovery and structural insight of a highly selective protein kinase inhibitor hit through click chemistry

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