New nicotinamide-thiadiazol hybrids as VEGFR-2 inhibitors for breast cancer therapy: design, synthesis and <i>in silico</i> and <i>in vitro</i> evaluation.

ABSTRACT: Vascular endothelial growth factor receptor-2 (VEGFR-2) is a key regulator of tumor angiogenesis and has become an important target in anticancer drug development. In this study, novel nicotinamide-thiadiazol hybrids were synthesized and evaluated for their anti-breast cancer potential through VEGFR-2 inhibition. The compounds were assessed in vitro for their cytotoxicity against MDA-MB-231 and MCF-7 cell lines. Among the nicotinamide-thiadiazol hybrids, 7a exhibited the most potent anticancer activity, with IC₅₀ values of 4.64 ± 0.3 μM in MDA-MB-231 and 7.09 ± 0.5 μM in MCF-7, showing comparable efficacy to sorafenib. VEGFR-2 inhibition assays confirmed strong inhibitory potential with an IC₅₀ of 0.095 ± 0.05 μM. In vitro cell cycle analysis indicated t

SUBMITTER: Elgammal WE 

PROVIDER: S-EPMC12056735 | biostudies-literature | 2025 Apr

REPOSITORIES: biostudies-literature