Synthesis, docking study & anticancer evaluation ofnovel 3-Phenyl-2-(3-aryl-phenyl-1H-pyrazol-4-yl) thiazolidin-4-ones

Bansal, Sumit and Kumar, Sharad and Choudhary, Anil and Tiwari, Amit and Joseph, Alex (2014) Synthesis, docking study & anticancer evaluation ofnovel 3-Phenyl-2-(3-aryl-phenyl-1H-pyrazol-4-yl) thiazolidin-4-ones. Indo Global Journal of Pharmaceutical Sciences, 4 (1). pp. 18-24. ISSN 2249-1023

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Abstract

On account of the reported anticancer activity of pyrazoles and thiazolidin-4-ones, we have designed and synthesized a series of novel 3-phenyl-2-(3-aryl-1-phenyl-1H-pyrazol-4-yl)thiazolidin-4-ones and investigated their COX-1 and COX-2 inhibition potential and also their in vitro cytotoxic activity by MTT assay. Amongst the tested compounds, the compound 3e was found to be most potent COX-2 inhibitor with IC50 value of 4.4 μM and showed promising anticancer potential with IC50 values of 14.78 μg/ml and 12.45 μg/ml against HT-29 and COLO-205 cancer cells, respectively, compared to 5-FU as a standard drug. The newly synthesized compounds were characterized by melting point, IR, 1H NMR, and MS analysis. Docking studies were performed on the active site of COX-1 and COX-2 enzymes.

Item Type: Article
Uncontrolled Keywords: Thiazolidin-4-ones; COX-2; colorectal cancer; docking.
Subjects: Pharmacy > MCOPS Manipal > Pharmaceutical Chemistry
Pharmacy > MCOPS Manipal > Pharmacology
Depositing User: KMC Manipal
Date Deposited: 29 Nov 2014 09:19
Last Modified: 29 Nov 2014 09:19
URI: http://eprints.manipal.edu/id/eprint/141164

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