Article
Structural optimization and structure-activity relationships of N2-(4-(4-Methylpiperazin-1-yl)phenyl)-N8-phenyl-9H-purine-2,8-diamine derivatives, a new class of reversible kinase inhibitors targeting both EGFR-activating and resistance mutations.
Journal of medicinal chemistry - 13 Dec 2012
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
Abstract excerpt
This paper describe the structural optimization of a hit compound, N2-(4-(4-methylpiperazin-1-yl)phenyl)-N8-phenyl-9H-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-activi...
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