Article
Design, synthesis and biological evaluation of selective inhibitors against the L858R/T790 M/C797S mutant EGFR kinase based on the scaffold of brigatinib.
European journal of medicinal chemistry - 15 Sept 2026
Ding Shi, Ding Haotian, Zhan Zhenzhen, Wang Jinpeng, Song Xinru, Wu Yuanyu, Wang Xin, Zheng Hanxue, Tang Zhongyu, Peng Xiaoqing, Wu Shaoting, Liu Ju, Shen Jiwei, Chen Ye
Abstract excerpt
Based on the scaffold of brigatinib, we designed and synthesized a series of novel EGFR tyrosine kinase inhibitors, followed by the evaluation of their activity against the L858R/T790 M/C797S mutant EGFR kinase. Compound 8c showed significantly higher inhibitory activity (IC50 = 0.48 nM) than brigatinib (IC50 = 3.41 nM), and preferred to inhibit the L858R/T790 M/C797S mutant EGFR kinase rather than other subtypes...
Read the complete abstract on PubMedTopics
Share this publication in a Topic to start or enrich a Post.