Coumarin derivatives as potential anticancer agents: Synthesis, antiproliferative activity, apoptosis, and molecular docking studies

This study presents the synthesis of a series of coumarin derivatives via efficient Ugi synthesis reactions, aimed at exploring their anti-proliferative properties. Out of the twelve synthesized derivatives, most exhibited significant anti-proliferative activity with minimal cytotoxic effects on normal MCF12A cells. Notably, compound 5i showed exceptional activity, achieving IC50 values of 17.69, 19.87, and 30.39 μM against HeLa, MCF-7, and A549 cell lines, respectively, comparable to Doxorubicin. Apoptosis assays revealed a pronounced dose-dependent effect, with apoptosis rates increasing to 22.75 % at 10 μM and 83.50 % at 40 μM. Additionally, molecular docking studies confirmed the compound's strong inhibitory potential against the anti-apoptotic Bcl-2 protein. These results highlight the promising role of compound 5i as an anticancer agent, warranting further exploration in therapeutic applications.