New Phenylaminopyrimidine (PAP) Anticancer Lead Compound withHigh Efficacy: Design, Synthesis, and in vitro Screening

Bulletin of the Korean chemical society

Dong Keun Han¹  In Tae Kim¹  So Ha Lee¹  Ibrahim Mustafa El Deeb¹ 

关键词: Phenylaminopyrimidines;    Kinase inhibitor;    Cancer cell-lines;    Selectivity;    Cancer;   

DOI  :  

学科分类：化学（综合）

来源: Korean Chemical Society

【 摘 要 】

Phenylaminopyrimidines represent a large group of new selective anticancer agents, the majority of which exert their action through the inhibition of specific kinases. In this study, a new series of N-substituted-2-aminopyrimidines has been designed and synthesized. A selected group of the synthesized derivatives was screened at a single dose concentration of 10 レM over a panel of 60 cancer cell-lines. Compound 12e has showed great inhibitory and strong lethal effect over almost all of the 60 cell-lines and accordingly was further tested in a 5-dose testing mode to determine its IC₅₀ values, where it showed great efficacies with intermediate potencies over the tested cell-lines. The compound was also tested over a panel of 52 kinases to explore its kinase inhibitory profile, and was found to be a selective but moderate inhibitor over FLT3 kinase.

【 授权许可】

Unknown