Abstract
Background: Three new series of coumarin derivatives 4a-e, 6a-d and 7a-d were synthesized and characterized by elemental analyses and spectral data including 2D NMR. All compounds 4a-e, 6a-d and 7a-d were evaluated for their in vitro antioxidant and anticancer activity against Hep-G2 hepatic cancer and MCF-7 breast cancer cell lines.
Method: Compounds 4c, 4e, 6d and 7c showed higher antioxidant activity (IC50 = 78, 20, 90 and 46 mu M, respectively) than the reference drug silymarin (IC50 = 76 mu M).
Results and Conclusion: However, the anticancer screening for the three series showed promising anticancer activity against hepatic Hep-G2 cancer cell line and compounds 4d, 4e, 6a and 6c (IC50 = 1890, 5327, 5715 and 10339 mu M, respectively) have more potent cytotoxic activity than cisplatin (IC50 = 11898 mu M). On the other hand, all compounds showed no anticancer activity against MCF-7 cell line except compound 6a with IC50 = 32441 mu M in comparison with cisplatin (IC50 = 15030 mu M).