Synthesis of phenoxyquinoline-pyrimidine hybrids demonstrates potent cytotoxicity in A549 and MCF-7 cells, suggesting potential as EGFR inhibitors.
This study designed and synthesized novel phenoxyquinoline-pyrimidine hybrids (7a-k) as potential EGFR inhibitors, with 7a and 7k exhibiting superior cytotoxicity (IC50 = 2.13 ± 0.18 µM and 1.01 ± 0.10 µM against A549 and MCF-7 cancer cell lines, respectively) compared to Gefitinib. Molecular docking revealed strong binding to EGFR-TKD (−9.4 kcal/mol for 7a), supported by key interactions with MET793 and LEU844, while SAR analysis highlighted methoxy groups as critical for activity. These findings introduce a new class of hybrid anticancer agents with validated mechanistic insights, offering a foundation for targeted therapy development.
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Nagarjuna et al. (2025) studied this question.
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