Article
Discovery of novel 2,4-diarylaminopyrimidine derivatives as potent and selective epidermal growth factor receptor (EGFR) inhibitors against L858R/T790M resistance mutation.
European journal of medicinal chemistry - 25 May 2018
Yan Qi, Chen Yuzhe, Tang Baiyou, Xiao Qiang, Qu Rong, Tong Linjiang, Liu Jian, Ding Jian, Chen Yi, Ding Ning, Tan Wenfu, Xie Hua, Li Yingxia
Abstract excerpt
A series of novel 2,4-diarylaminopyrimidine derivatives of AZD9291 were discovered as L858R/T790M mutant selective epidermal growth factor receptor (EGFR) inhibitors. The majority of these compounds exhibited moderate to excellent EGFR T790 M/L858R inhibitory activities and comparable anti-proliferative activities against double mutant over-expressed NCI-H1975 cells to that of AZD9291. The most promising...
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