Design, synthesis and biological evaluation of selective inhibitors against the L858R/T790M/C797S mutant EGFR kinase based on the scaffold of brigatinib

2026-05-01

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丁

丁实 (Shi Ding)

Haotian Ding

Zhenzhen Zhan

Jinpeng Wang

Xinru Song

Yuanyu Wu

Xin Wang

Hanxue Zheng

Zhongyu Tang

Xiaoqing Peng

Shaoting Wu

Ju Liu *

Jiwei Shen *

Ye Chen *

DOI：10.1016/j.ejmech.2026.118915

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Abstract

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• 8c showed better kinase inhibitory activity and selectivity than brigatinib. • 8c exhibited better antiproliferative activity and selectivity than brigatinib. • 8c concentration-dependently induced the apoptotic process of tumor cells. • The combination mode of 8c was deeply analyzed by docking analysis.

Keywords:

kinase inhibitory activity

antiproliferative activity

apoptotic process

molecular docking

EGFR kinase inhibitors

Design, synthesis and biological evaluation of selective inhibitors against the L858R/T790M/C797S mutant EGFR kinase based on the scaffold of brigatinib

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