Article
Discovery of a potent EGFR and ALK dual mutation inhibitor containing N-(3-((4-((2-(cyclopropylsulfinyl)phenyl)amino)pyrimidin-2-yl)amino) phenyl)acrylamide scaffold.
Bioorganic chemistry - 1 Dec 2022
Li Wei, Yao Han, Gu Chenxi, Ren Yuanyuan, Liu Jiadai, An Baijiao, Hu Wenhao, Li Xingshu, Chan Albert S C
Abstract excerpt
A series of EGFR and ALK dual inhibitors containing sulfoxide and cyclopropyl groups were designed and synthesized. The lead compound 8a showed a significant activity against EGFR and ALK in both the enzymatic and cellular assays. The study of anti-tumor mechanism indicated that 8a could effectively block the phosphorylation of EGFR and ALK proteins, so as to effectively inhibiting the proliferation and inducing...
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