Novel 2, 4-diarylaminopyrimidine analogues (DAAPalogues) showing potent c-MET/ALK multikinase inhibitory activities

Z Liu, J Ai, X Peng, Z Song, K Wu, J Zhang…

Index: Liu, Zhiqing; Ai, Jing; Peng, Xia; Song, Zilan; Wu, Kui; Zhang, Jing; Yao, Qizheng; Chen, Yi; Ji, Yinchun; Yang, Yanhong; Geng, Meiyu; Zhang, Ao ACS Medicinal Chemistry Letters, 2014 , vol. 5, # 4 p. 304 - 308

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Citation Number: 9

Abstract

By repurposing a typical dopamine D1/D5 receptor agonist motif, C1-substituted-N 3- benzazepine or benzazecine, into the classical RTK inhibitor 2, 4-diaminopyrimidine skeleton, a series of new 2, 4-diarylaminopyrimidine analogues (DAAPalogues) were developed. Compounds 7 and 8a were identified possessing high potency against both c- Met and ALK kinases. Compound 8a displayed appreciable antitumor efficacy at the dose ...