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

Gurupadaswamy, H. D. ; Girisha, V. ; Kavitha, C. V. ; Raghavan, Sathees C. ; Khanum, Shaukath Ara (2013) Synthesis and evaluation of 2, 5-di (4-aryloylaryloxymethyl)-1, 3, 4-oxadiazoles as anti-cancer agents European Journal of Medicinal Chemistry, 63 . pp. 536-543. ISSN 0223-5234

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Official URL: http://www.sciencedirect.com/science/article/pii/S...

Related URL: http://dx.doi.org/10.1016/j.ejmech.2013.02.040

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 lines (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 μM). 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.

Item Type:Article
Source:Copyright of this article belongs to Elsevier Science.
Keywords:1,3,4-Oxadiazoles; Cytotoxicity; Apoptosis
ID Code:103964
Deposited On:11 Apr 2017 16:18
Last Modified:11 Apr 2017 16:18

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