Design, synthesis and biological evaluation of novel 6-alkenylamides substituted of 4-anilinothieno [2, 3-d] pyrimidines as irreversible epidermal growth factor receptor …

…, W Yang, L Tong, R Qu, H Jiang, J Ding, H Xie…

文献索引：Ji, Xun; Peng, Ting; Zhang, Xu; Li, Jian; Yang, Wei; Tong, Linjiang; Qu, Rong; Jiang, Hualiang; Ding, Jian; Xie, Hua; Liu, Hong Bioorganic and Medicinal Chemistry, 2014 , vol. 22, # 7 p. 2366 - 2378

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被引用次数: 14

摘要

Abstract A novel series of 6-alkenylamides of 4-anilinothieno [2, 3-d] pyrimidine derivatives was designed, synthesized and evaluated as irreversible inhibitors of the epidermal growth factor receptor (EGFR). Most of the compounds exhibited good potency against EGFR wild type (EGFR wt) and EGFR T790M/L858R. Among these, the half-maximal inhibitory concentration (IC 50) values of 17 compounds against EGFR wt were less than 0.020 μM, ...