Synthesis of new coumarin tethered isoxazolines as potential anticancer agents

Lingaraju, G. S. and Balaji, K. S. and Jayarama, S. and Anil, S. M. and Kiran, K. R. and Sadashiva, M. P. (2018) Synthesis of new coumarin tethered isoxazolines as potential anticancer agents. Bioorganic and Medicinal Chemistry Letters, 28 (23-24). pp. 3606-3612.

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A series of new coumarin tethered isoxazolines (7a-l) were synthesized and evaluated for their cytotoxic potency against human melanoma cancer cell line (UACC 903) as well as fibroblast normal cell line (FF2441). Preliminary results revealed that some of these coumarin tethered isoxazolines 7b, 7c, 7f and 7j exhibited significant antiproliferative effect against human melanoma cancer (UACC 903) with IC50 values of 8.8, 10.5, 9.2 and 4.5 μM respectively. However, compound 7c was non-toxic to normal human cells at the tested concentration. Further, we have chosen compound 7c to check its efficacy in Ehrlich Ascites Carcinoma animal model in-vivo for its antitumor and antiangiogenic properties. Our lead compound significantly reduced the cell viability, body weight, ascites volume and downregulated the formation of neovasculature such as regression of tumor volume. The present study indicates the scope of developing into potent anticancer drug in near future.

Item Type: Article
Subjects: C Chemical Science > Chemistry
Divisions: Department of > Chemistry
Depositing User: Manjula P Library Assistant
Date Deposited: 11 Jan 2021 06:26
Last Modified: 11 Jan 2021 06:26

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