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Article

Novel EGFR inhibitors against resistant L858R/T790M/C797S mutant for intervention of non-small cell lung cancer.

European journal of medicinal chemistry - 5 Nov 2024

Wang Xiaoxue, Qin Zhongxiang, Qiu Wenrui, Xu Kejia, Bai Yuting, Zeng Beilei, Ma Yakun, Yang Shuang, Shi Yi, Fan Yan

Abstract excerpt

To overcome C797S mutation, the latest and most common resistance mechanism in the clinical treatment of third-generation EGFR inhibitor, a novel series of substituted 6-(2-aminopyrimidine)-indole derivatives were designed and synthesized. Through the structure-activity relationship (SAR) study, compound 11eg was identified as a novel and potent EGFR L858R/T790M/C797S inhibitor (IC50 = 0.053 μM) but had a weak...

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Identifiers

PMID: 39094277
DOI: 10.1016/j.ejmech.2024.116711

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-08.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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