Discovery and optimization of 4-anilinoquinazoline derivatives spanning ATP binding site and allosteric site as effective EGFR-C797S inhibitors.

doi:10.1016/j.ejmech.2022.114856

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Article

Discovery and optimization of 4-anilinoquinazoline derivatives spanning ATP binding site and allosteric site as effective EGFR-C797S inhibitors.

European journal of medicinal chemistry - 15 Dec 2022

Dou Dou, Wang Jie, Qiao Yunjin, Wumaier Gulinuer, Sha Wenjie, Li Wenjie, Mei Wenyi, Yang Tingyuan, Zhang Chen, He Huan, Wang Caolin, Chu Linna, Sun Baihui, Su Rongrong, Ma Xiangyu, Gong Mengdie, Xie Lijuan, Jiang Wenzhe, Diao Yanyan, Zhu Lili, Zhao Zhenjiang, Chen Zhuo, Xu Yufang, Li Shengqing, Li Honglin

Abstract excerpt

Epidermal growth factor receptor (EGFR) is an effective drug target for the treatment of non-small cell lung cancer (NSCLC). However, a tertiary point mutation (C797S) at the ATP binding pocket of the EGFR induces resistance to the third-generation EGFR inhibitors, due to the loss of covalent interaction with Cys797. Here, we designed a series of 4-anilinoquinazoline derivatives that simultaneously occupied the...

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PMID: 36279692
DOI: 10.1016/j.ejmech.2022.114856

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