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Design, synthesis and biological evaluation of structurally new 4-indolyl quinazoline derivatives as highly potent, selective and orally bioavailable EGFR inhibitors.

Bioorganic chemistry - 1 Jan 2024

He Pengxing, Du Linna, Dai Qingqing, Li Guobo, Yu Bin, Chang Linlin

Abstract excerpt

Targeting the epidermal growth factor receptor (EGFR) has been recognized as an effective strategy for treating non-small-cell lung cancer (NSCLC). Although several representative EGFR inhibitors have been approved for clinical use, it is highly desirable to develop highly potent and selective EGFR inhibitors with novel scaffolds because of the occurrence of acquired resistance after treatment. Here we first...

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PMID: 37984101
DOI: 10.1016/j.bioorg.2023.106970

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