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Article

Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors.

European journal of medicinal chemistry - 5 Apr 2022

Tang Qidong, Peng Ting, Hu Jie, Zhang Tao, Chen Pengqin, Chen Daoxing, Wang Yunjie, Chen Lingfeng, Tong Linjiang, Chen Yi, Xie Hua, Liang Guang

Abstract excerpt

Pan-HER inhibitors exhibit extensive biological activity and offer unique advantages and usually bind to targets in an irreversible manner. Owing to the off-target toxicity of irreversible inhibitors, reversible pan-HER inhibitors are desirable. Herein, we describe the process of N-(ring structure fused phenyl)quinazoline-4-amine-based design, synthesis, and biological evaluation of pan-HER inhibitors in vitro...

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PMID: 35259690
DOI: 10.1016/j.ejmech.2022.114249

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