Design, Synthesis, Antioxidant and Anticancer Activity of New Coumarin Derivatives Linked with Thiazole, Isoxazole or Pyrazole Moiety

Author(s): Khaled R. A. Abdellatif*, Mohamed A. Abdelgawad, Heba A. H. Elshemy, Nesma M. Kahk, Dalia M. El Amir

Journal Name: Letters in Drug Design & Discovery

Volume 14 , Issue 7 , 2017

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Graphical 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 μM, respectively) than the reference drug silymarin (IC50 = 76 μM).

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 μM, respectively) have more potent cytotoxic activity than cisplatin (IC50 = 11898 μM). On the other hand, all compounds showed no anticancer activity against MCF-7 cell line except compound 6a with IC50 = 32441 μM in comparison with cisplatin (IC50 = 15030 μM).

Keywords: Coumarin, pyrazole, isoxazole, thiazole, antioxidant, anticancer.

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Article Details

Year: 2017
Published on: 29 June, 2017
Page: [773 - 781]
Pages: 9
DOI: 10.2174/1570180813666161026153743
Price: $65

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