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Quinazoline-based fourth-generation EGFR tyrosine kinase inhibitors to overcome C797S-mediated resistance in non-small cell lung Cancer (NSCLC).

Bioorganic chemistry - 1 Oct 2025

Patil Bhatu R, Pawara Kisan, Shaikh Matin, Ahmed Faizan, Patil Chandragouda R, Gawli Chandrakant S, Kundu Chanakya Nath, Das Biswajit, Ahmad Iqrar, Patel Harun M

Abstract excerpt

The emergence of resistance mutations, particularly C797S, in epidermal growth factor receptor tyrosine kinase (EGFR-TK) has significantly limited the long-term efficacy of Osimertinib in non-small cell lung cancer (NSCLC). In this study, we designed and evaluated a series of quinazoline derivatives targeting the triple mutant EGFR (L858R/T790M/C797S). Among them, compound 8d exhibited the highest potency against...

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Share to Drug Resistance, Neoplasm
Share to Drug Screening Assays, Antitumor

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

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Identifiers

PMID: 40966776
DOI: 10.1016/j.bioorg.2025.108991

Genes

EGFR
C2

Variants

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 2 Sept 2026.

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