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Article

Pan-EGFR inhibitor targeting EGFR 19del, L858R/T790M and C797S triple-mutations: Design, synthesis, and pharmacological evaluation.

Bioorganic chemistry - 1 Sept 2025

Wang Luhong, Xie Fei, Li Shujing, Guo Guanglu, Song Qiyu, Yuan Xinyu, Kang Jie, Li Yulin, Wang Aoli, Wu Huijian, Xu Youjun

Abstract excerpt

Acquired resistance mediated by the EGFR C797S mutation remains a critical barrier in the treatment of non-small cell lung cancer (NSCLC), reducing the effectiveness of third-generation EGFR inhibitors that target T790M-containing mutations. In this study, novel 2,4-diarylamino pyrimidine derivatives were identified and characterized as pan-mutant EGFR tyrosine kinase inhibitors. Compound D10 potently inhibited...

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Identifiers

PMID: 40876225
DOI: 10.1016/j.bioorg.2025.108878

Genes

EGFR
F3

Variants

Provenance

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