Article
1-Methyl-3-((4-(quinolin-4-yloxy)phenyl)amino)-1H-pyrazole-4-carboxamide derivatives as new rearranged during Transfection (RET) kinase inhibitors capable of suppressing resistant mutants in solvent-front regions.
European journal of medicinal chemistry - 15 Dec 2022
Zhang Yunong, Chan Shinpan, He Rui, Liu Yiling, Song Xiaojuan, Tu Zheng-Chao, Ren Xiaomei, Zhou Yang, Zhang Zhang, Wang Zhen, Zhou Fengtao, Ding Ke
Abstract excerpt
REarranged during Transfection (RET) is a validated target for anticancer drug discovery and two selective RET inhibitors were approved by US FDA in 2020. However, acquired resistance mediated by secondary mutations in the solvent-front region of the kinase (e.g. G810C/S/R) becomes a major challenge for selective RET inhibitor therapies. Herein, we report a structure-based design of...
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