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Article

Design, synthesis and biological evaluation of novel tumor hypoxia-activated EGFR tyrosine kinase inhibitors.

Bioorganic chemistry - 1 Dec 2022

Jia Tingting, Miao Ruoyang, Lin Jiaohua, Zhang Chong, Zeng Linghui, Zhang Jiankang, Shao Jiaan, Pan Zongfu, Wang Haiping, Zhu Huajian, Cheng Weiyan

Abstract excerpt

Hypoxia is widespread in solid tumors, such as NSCLC, and has become a very attractive target. On the basis of AZD9291 scaffold, novel hypoxia-targeted EGFR inhibitors without the acrylamide warhead but containing hypoxic reductive activation groups were described. Among them, compound JT21 exhibited impressive inhibitory activity (IC50 = 23 nM) against EGFRL858R/T790M and displayed about 21-fold inhibitory...

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Identifiers

PMID: 36115310
DOI: 10.1016/j.bioorg.2022.106138

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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