Article
Identification and anti-tumor evaluation of 3-acyl-indol-based 2,4-diarylaminopyrimidine analogues as potent ALK inhibitors capable of overcoming drug-resistant mutants.
European journal of medicinal chemistry - 5 Aug 2022
Guo Ming, Wang Hao, Yang Jing, Wang Xinyu, Zhang Jiahao, Liu Shuyu, Wei Shangfei, Jiang Nan, Zhai Xin
Abstract excerpt
A series of novel 2,4-diarylaminopyrimidine analogues (G-1∼G-8 and I-1∼I-24) were rationally designed by incorporating 2-alkyl-3-acyl-1H-indol fragment to interact with the hydrophobic region of the intractable ALKG1202R mutant. Wherein, compound I-24 bearing a 2-methyl-3-dimethylformamido-1H-indol moiety was identified as the most promising ALK inhibitor with IC50 values below 4 nM against ALKWT, ALKL1196M and...
Read the complete abstract on PubMedTopics
Share this publication in a Topic to start or enrich a Post.