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Antiproliferative and tumor inhibitory studies of 2,3 disubstituted 4-thiazolidinone derivatives

Kumar, Kothanahally S Sharath and Hanumappa, Ananda and Vetrivel, Maruthai and Hegde, Mahesh and Girish, Yarabhally R and Byregowda, Thinnali R and Rao, Suguna and Raghavan, Sathees C and Rangappa, Kanchugarakoppal S (2015) Antiproliferative and tumor inhibitory studies of 2,3 disubstituted 4-thiazolidinone derivatives. In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 25 (17). pp. 3616-3620.

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Official URL: http://dx.doi.org/10.1016/j.bmcl.2015.06.069

Abstract

4-Thiazolidinone derivatives were synthesized using T3P (R)-DMSO media as a cyclodehydrating agent. All the molecules were tested for their cytotoxicity against leukemic cell lines. The compound 3-(4-bromophenyl)-2-(4-(dimethylamino)phenyl)thiazolidin-4-one (4e) with electron donating substituent at para position of phenyl ring displayed considerable cytotoxicity against Reh and Nalm6 cells with an IC50 value of 11.9 and 13.5 mu M, respectively. Furthermore, the compound 4e tested for tumor regression studies induced by EAC in Swiss albino mouse. Both in vitro and in vivo results suggested significant antiproliferative activity of compound 4e in Reh cells and mouse tumor tissue treated with compound 4e showed multifocal areas of necrosis and numerous number of apoptotic cells. (C) 2015 Elsevier Ltd. All rights reserved.

Item Type: Journal Article
Publication: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Publisher: PERGAMON-ELSEVIER SCIENCE LTD
Additional Information: Copy right for this article belongs to the PERGAMON-ELSEVIER SCIENCE LTD, THE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLAND
Keywords: 4-Thiazolidinone; T3P; Reh; EAC; Tumor regression
Department/Centre: Division of Biological Sciences > Biochemistry
Date Deposited: 11 Sep 2015 04:18
Last Modified: 11 Sep 2015 04:18
URI: http://eprints.iisc.ac.in/id/eprint/52311

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