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Article

Fragment-based modification of 2,4-diarylaminopyrimidine derivatives as ALK and ROS1 dual inhibitors to overcome secondary mutants.

Bioorganic & medicinal chemistry - 15 Oct 2020

Zhu Minglin, Li Wei, Zhao Tianming, Chen Yuxiang, Li Tong, Wei Shangfei, Guo Ming, Zhai Xin

Abstract excerpt

In order to explore novel ALK and ROS1 dual inhibitors capable of overcoming crizotinib-resistant mutants, two series of 2,4-diarylaminopyrimidine derivatives were designed, synthesized and evaluated for their in vitro cytotoxic activity. In this work, we retained the 2,4-diarylaminopyrimidine scaffold and derivatize the DAAP scaffold with sulfonyl and acrylamide moieties to extend the structure-activity...

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Identifiers

PMID: 33069075
DOI: 10.1016/j.bmc.2020.115719

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