Multi-targeted azacoumarin-cyanocinnamate hybrids induce G₂/M arrest and apoptosis <i>via</i> tubulin, and COX-2/VEGFR modulation: insights from <i>in vitro</i> mechanistic basis and <i>in vivo</i> validation.

ABSTRACT: Cancer remains a significant global health concern, with breast cancer ranking among the leading causes of cancer-related mortality in women. In pursuit of multi-targeted anticancer agents, we designed and synthesized a novel series of 7-hydroxy azacoumarin-α-cyanocinnamate hybrids and evaluated their therapeutic potential through comprehensive in vitro and in vivo studies. Structural characterization was confirmed using NMR, IR, and elemental analysis. Among the synthesized compounds, compound 7 exhibited the most potent cytotoxic activity against MCF-7 cells (IC₅₀ = 7.65 μM) and MDA-MB-231 (IC₅₀ = 9.7 ± 1.15 μM), with notable selectivity over non-tumorigenic MCF-10A cells (IC₅₀ = 52.02 μM), as compared to the reference drug doxorubicin. Mech

SUBMITTER: El-Zend MA 

PROVIDER: S-EPMC12461739 | biostudies-literature | 2025 Aug

REPOSITORIES: biostudies-literature