Structural Optimization and Structure–Activity Relationships of N 2-(4-(4-Methylpiperazin-1-yl) phenyl)-N 8-phenyl-9 H-purine-2, 8-diamine Derivatives, a New Class of …

…, L Zhong, RL Zheng, Y Xu, P Ji, CH Zhang…

文献索引：Yang, Jiao; Wang, Li-Jiao; Liu, Jing-Jing; Zhong, Lei; Zheng, Ren-Lin; Xu, Yong; Ji, Pan; Zhang, Chun-Hui; Wang, Wen-Jing; Lin, Xing-Dong; Li, Lin-Li; Wei, Yu-Quan; Yang, Sheng-Yong Journal of Medicinal Chemistry, 2012 , vol. 55, # 23 p. 10685 - 10699

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被引用次数: 24

摘要

This paper describe the structural optimization of a hit compound, N 2-(4-(4-methylpiperazin- 1-yl) phenyl)-N 8-phenyl-9 H-purine-2, 8-diamine (1), which is a reversible kinase inhibitor targeting both EGFR-activating and drug-resistance (T790M) mutations but has poor binding affinity. Structure–activity relationship studies led to the identification of 9-cyclopentyl-N 2-(4- (4-methylpiperazin-1-yl) phenyl)-N 8-phenyl-9 H-purine-2, 8-diamine (9e) that exhibits ...