Article
Discovery of 4-methyl-N-(4-((4-methylpiperazin- 1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((6-(pyridin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl)-oxy)benzamide as a potent inhibitor of RET and its gatekeeper mutant.
European journal of medicinal chemistry - 1 Dec 2020
Li Xiaoyang, Su Jingyi, Yang Yanru, Lian Wenhua, Deng Zhou, Yang Zaiyou, Chen Guyue, Zhang Baoding, Dong Chao, Liu Xueyan, Li Li, Wang Zheng, Hu Zhiyu, Xu Qingyan, Deng Xianming
Abstract excerpt
The receptor tyrosine kinase rearranged during transfection (RET) plays pivotal roles in several cancers, including thyroid carcinoma and non-small cell lung cancer (NSCLC). Currently, there are several FDA-approved RET inhibitors, but their indication is limited to thyroid cancer, and none can overcome their gatekeeper mutants (V804L and V804M). Here, we report the discovery of 9x representing a new chemotype of...
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