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.
Letters in Drug Design & Discovery
Title:Design, Synthesis, Antioxidant and Anticancer Activity of New Coumarin Derivatives Linked with Thiazole, Isoxazole or Pyrazole Moiety
Volume: 14 Issue: 7
Author(s): Khaled R. A. Abdellatif*, Mohamed A. Abdelgawad, Heba A. H. Elshemy, Nesma M. Kahk and Dalia M. El Amir
Affiliation:
- Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Beni-Suef University, Beni- Suef,Egypt
Keywords: Coumarin, pyrazole, isoxazole, thiazole, antioxidant, anticancer.
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).Export Options
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Cite this article as:
Abdellatif R. A. Khaled*, Abdelgawad A. Mohamed, Elshemy A. H. Heba, Kahk M. Nesma and El Amir M. Dalia, Design, Synthesis, Antioxidant and Anticancer Activity of New Coumarin Derivatives Linked with Thiazole, Isoxazole or Pyrazole Moiety, Letters in Drug Design & Discovery 2017; 14 (7) . https://dx.doi.org/10.2174/1570180813666161026153743
DOI https://dx.doi.org/10.2174/1570180813666161026153743 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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