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Synthesis and antiproliferative activity of imidazo2,1-b]1,3,4]thiadiazole derivatives

Kumar, Sujeet and Gopalakrishnan, Vidya and Hegde, Mahesh and Rana, Vivek and Dhepe, Sharad S and Ramareddy, Sureshbabu A and Leoni, Alberto and Locatelli, Alessandra and Morigi, Rita and Rambaldi, Mirella and Srivastava, Mrinal and Raghavan, Sathees and Karki, Subhas S (2014) Synthesis and antiproliferative activity of imidazo2,1-b]1,3,4]thiadiazole derivatives. In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 24 (19). pp. 4682-4688.

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Official URL: http://dx.doi.org/10.1016/j.bmcl.2014.08.032

Abstract

A series of 2,5,6-substituted imidazo2,1-b]1,3,4]thiadiazole derivatives have been prepared and were tested for antiproliferative activity on cancer cells at the National Cancer Institute. Results showed that molecules with a benzyl group at position 2, exhibited an increase in activity for the introduction of a formyl group at the 5 position. The compound 2-benzyl-5-formyl-6-(4-bromophenyl)imidazo 2,1-b]1,3,4]thiadiazole 22 has been chosen for understanding the mechanism of action by various molecular and cellular biology studies. Results obtained from cell cycle evaluation analysis, analysis of mitochondrial membrane potential and Annexin V-FITC by flow cytometric analysis, ROS production and expression of apoptotic and DNA-repair proteins suggested that compound 22 induced cytotoxicity by activating extrinsic pathway of apoptosis, however, without affecting cell cycle progression. (C) 2014 Elsevier Ltd. All rights reserved.

Item Type: Journal Article
Additional Information: Copyright for this article belongs to the PERGAMON-ELSEVIER SCIENCE LTD, THE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLAND.
Keywords: Antiproliferative agents; Imidazo2,1-b]1,3,4]thiadiazoles; Cell-based screening assay; Hollow fiber assay; Acute toxicity; Apoptosis
Department/Centre: Division of Biological Sciences > Biochemistry
Depositing User: Id for Latest eprints
Date Deposited: 08 Nov 2014 05:25
Last Modified: 08 Nov 2014 05:25
URI: http://eprints.iisc.ac.in/id/eprint/50195

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