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

Eur J Med Chem. 2013 May:63:536-43. doi: 10.1016/j.ejmech.2013.02.040.

H D Gurupadaswamy ¹, V Girish, C V Kavitha, Sathees C Raghavan, Shaukath Ara Khanum

Affiliations

Affiliation

1 Department of Chemistry, Yuvaraja's College Mysore, University of Mysore, Mysore 570 006, India.

PMID: 23535322 DOI: 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.

Name
Email *

	Sorry, but the email address you supplied was invalid.