Synthesis and antiproliferative activities of novel 4H-chromene-5-one derivatives synthesized from cyclohexane-1,3-dione

This study presents the novel synthesis of approximately 54 derivatives of 4H-chromene-5-one and evaluates their anticancer activity. The key intermediates, 7,8-dihydro-2,4-diphenyl-4H-chromen-5(6H)-one derivatives (5a–i), were synthesized via multicomponent reactions to yield the target compounds. Structural characterization of all synthesized derivatives was confirmed using various spectroscopic techniques. The antiproliferative activity of these heterocyclic compounds was assessed against six human cancer cell lines: A549, HT-29, MKN-45, U87MG, SMMC-7721, and H460. A significant number of the tested compounds exhibited strong cytotoxic effects across all cell lines. Notably, many compounds demonstrated superior cytotoxicity compared to the reference drug Foretinib. KEY WORDS: Multi-component reactions, Thiophene derivative, Anticancer activity, 7,8-Dihydro-2,4-diphenyl-4H-chromen-5(6H)-one Bull. Chem. Soc. Ethiop. 2026, 40(4), 861-877. DOI: https://dx.doi.org/10.4314/bcse.v40i4.10