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
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.
