Synthesis and evaluation of 2,5-di(4-aryloylaryloxymethyl)-1,3,4-oxadiazoles as anti-cancer agents

Gurupadaswamy, HD and Girish, V and Kavitha, CV and Raghavan, Sathees C and Khanum, Shaukath Ara (2013) Synthesis and evaluation of 2,5-di(4-aryloylaryloxymethyl)-1,3,4-oxadiazoles as anti-cancer agents. In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 63 . pp. 536-543.

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Abstract

A series of 2,5-di(4-aryloylaryloxymethyl)-1,3,4-oxadiazoles 9a-j were obtained via multistep synthesis from hydroxybenzophenones 4a-e. The cytotoxicity of compounds 9a-j was evaluated against human leukemia cell lilies (K562 and CEM). The compounds exhibited moderate to good anti-cancer activity with compounds 9b and 9i having a chloro group exhibiting the best activity (IC50 = 10 mu M). Compound 9i exhibited activity against both the cell lines and 9b only exhibited activity against CEM. Further, a lactate dehydrogenase (LDH) assay and DNA fragmentation studies of the compounds 9a-j were also performed. (C) 2013 Elsevier Masson SAS. All rights reserved.

Item Type:	Journal Article
Publication:	EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Publisher:	ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
Additional Information:	Copyright for this article belongs to Science Direct
Keywords:	1,3,4-Oxadiazoles; Cytotoxicity; Apoptosis
Department/Centre:	Division of Biological Sciences > Biochemistry
Date Deposited:	25 Oct 2013 06:48
Last Modified:	25 Oct 2013 06:48
URI:	http://eprints.iisc.ac.in/id/eprint/47528

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