2-(4-Chlorobenzyl)-6-arylimidazo2,1-b]1,3,4]thiadiazoles: Synthesis, cytotoxic activity and mechanism of action

Kumar, Sujeet and Hegde, Mahesh and Gopalakrishnan, Vidya and Renuka, Vinaya Kumar and Ramareddy, Sureshbabu A and De Clercq, Erik and Schols, Dominique and Narasimhamurthy, Anil Kumar Gudibabande and Raghavan, Sathees C and Karki, Subhas S (2014) 2-(4-Chlorobenzyl)-6-arylimidazo2,1-b]1,3,4]thiadiazoles: Synthesis, cytotoxic activity and mechanism of action. In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 84 . pp. 687-697.

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Abstract

The cytotoxic activity of a new series of 2-(4'-chlorobenzyl)-5,6-disubstituted imidazo2,1-b]1,3,4]wthiadiazoles against different human and murine cancer cell lines is reported. Among the tested compounds, two derivatives namely 2-(4-chlorobenzyl)-6-(2-oxo-2H-chromen-3-yl)imidazo2,1-1)]1,3,4]th iadiazole-5-carbaldehyde 4i and 2-(4-chlorobenzyl)-6-(2-oxo-2H-chromen-3-ypimidazo2,1-1)]1,3,4]thi adiazol-5-yl thiocyanate 5i emerged as the most potent against all the cell lines. To investigate the mechanism of action, we selected compounds 4i for cell cycle study, analysis of mitochondrial membrane potential and Annexin V-FITC flow cytometric analysis and DNA fragmentation assay. Results showed that 4i induced cytotoxicity by inducing apoptosis without arresting the cell cycle. (C) 2014 Elsevier Masson SAS. All rights reserved.

Item Type:	Journal Article
Publication:	EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Additional Information:	Copy right for this article belongs to the ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER, 23 RUE LINOIS, 75724 PARIS, FRANCE
Department/Centre:	Division of Biological Sciences > Biochemistry
Date Deposited:	15 Oct 2014 05:01
Last Modified:	15 Oct 2014 05:01
URI:	http://eprints.iisc.ac.in/id/eprint/50015

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