Synthesis, Docking Study & Anticancer Evaluation of Novel 3-Phenyl- 2-(3-aryl-1-phenyl-1H-pyrazol-4-yl)thiazolidin-4-ones
نویسندگان
چکیده
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 COX2 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, 1 H NMR, and MS analysis. Docking studies were performed on the active site of COX-1 and COX-2 enzymes. © 2011 IGJPS. All rights reserved.
منابع مشابه
A facile iodine(III)-mediated synthesis of 3-(3-aryl-1-phenyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridines via oxidation of 2-((3-aryl-1-phenyl-1H-pyrazol-4-yl)methylene)-1-(pyridin-2-yl)hydrazines and their antimicrobial evaluations
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