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Design, synthesis, and biological evaluation of quinazoline–benzohydrazide and quinazoline–benzothiazole hybrids uncovering a dual EGFR/VEGFR-2 inhibitor with pronounced cytotoxic activity against triple-negative breast Cancer
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DOI：10.1016/j.bmc.2025.118515.png)
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Abstract
En 中文
• Series of quinazoline-hybrids (7a–f) and (10a–f) have been synthesized as EGFR and VEGFR-2 inhibitors. • Compound 7a was the most potent hybrid against four cancer cell lines, HeLa, HePG-2, MCF-7, and HCT-116. • Compound 7a exerted significant cytotoxic effects against triple-negative breast cancer (TNBC) MDA-MB-231 cells. • Compound 7a showed multi-target activity against EGFR and VEGFR-2 enzymes. • Compound 7a caused cell cycle arrest at G0/G1 phase and induced apoptosis of MDA-MB-231 cells. • Apoptotic profiling of compound 7a further indicated a substantial upregulation of Bax and downregulation of Bcl-2. • Molecular Docking study revealed that 7a hybrid represented appropriate binding with the two enzymes active sites.
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B
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3
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1.7W
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2.7W
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Cited Papers