Why the study?
Breast cancer causes substantial mortality, and elevated VEGFR-2 promotes cancer cell growth and survival, prompting the assessment of pyridine-containing acyl hydrazones as anticancer agents targeting this pathway.
Compound 12, a novel pyridine containing acylhydrazone, demonstrated superior in vitro cytotoxicity against MCF-7 breast cancer cells and stronger in silico binding to VEGFR-2 compared to reference drugs.
Caution against clinical use in breast cancer; leaves open further development of these VEGFR-2 inhibitors.
Among different types of cancer, breast cancer is responsible for 0.67 million deaths in 2022. Numerous cancer cells exhibit elevated Vascular Endothelial Growth Factor Receptor – 2 (VEGFR-2) expression, which triggers a series of biological reactions that enhance cell growth, survival and proliferation. Commercially available drugs and medicinal chemistry frequently use heterocycles as structural components to target many biological pathways and cause cancer cells to die. The assessment of pyridine containing acyl hydrazones as anti-cancer agents is presented here. The compounds 7a , 7b and 12 have shown inhibitory activities in 0.668, 0.783 and 0.627 µM against MCF-7 cells in Alamar Blue assay. Among these, compound 12 is the lead candidate, which performed better than reference drugs Doxorubicin (0.73 µM) and Tamoxifen (1.75 µM). The structure based molecular interaction studies of 12 to VEGFR-2 exhibited a significant binding energy of −7.24 kcal/mol, which is more efficient than that of Axitinib (-6.85 kcal/mol). • Synthesis of acylhydrazones. • Cytotoxic studies. • Docking studies.
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Shivakumar et al. (2025) studied this question.
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