Synthesis, characterization, anticancer, and antioxidant activity of some new thiazolidin-4-ones in MCF-7 cells

Pai, KSR and Maliyakkl, Naseer (2013) Synthesis, characterization, anticancer, and antioxidant activity of some new thiazolidin-4-ones in MCF-7 cells. Medicinal Chemistry Research, 22 (2). pp. 758-767. ISSN 1054-2523

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Abstract

There are limited studies centring on the potential of thiazolidin-4-ones as anticancer agents. In this study, a new series of 2-(3-substituted-1H-pyrazol-4-yl)-3- (3-substituted-5-sulfanyl-1,2,4-triazol-4-yl)-1,3-thiazolidin- 4-one (4a–o) have been synthesized by cyclo-condensation reaction of 5-substituted-4-[(3-substituted-1H-pyrazol-4- ylmethylidene)amino]-2H-1,2,4-triazole-3-thione (3a–o) and thioglycolic acid. The structures of all the synthesized compounds were confirmed by elemental analysis, spectral techniques like IR, 1H NMR, and mass spectroscopy. Few compounds exhibited dose-dependent cytotoxic effect in MTT assay in human breast cancer (MCF-7) cells. Apoptotic degradation of DNA due to action of potent thiazolidin- 4-ones was analysed by agarose gel electrophoresis and visualized by ethidium bromide staining (comet assay). A concentration-dependent increase in tail length and olive tail moment was observed when treated with thiazolidin-4- ones. In vitro antioxidant studies like DPPH and ABTSfree radical scavenging assays-indicated moderate activity of thiazolidin-4-ones.

Item Type: Article
Uncontrolled Keywords: Thiazolidin-4-one; Cytotoxicity; DNA fragmentation; Antioxidant activity
Subjects: Pharmacy > MCOPS Manipal > Pharmacology
Depositing User: KMC Manipal
Date Deposited: 09 Feb 2013 04:17
Last Modified: 09 Feb 2013 04:17
URI: http://eprints.manipal.edu/id/eprint/78306

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