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

Chemistry

Medicinal Chemistry

Author(s): Gurupadaswamy HD, Girish V, Kavitha CV, Raghavan SC, Khanum SA

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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 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. Copyright © 2013 Elsevier Masson SAS. All rights reserved. This article was published in Eur J Med Chem and referenced in Medicinal Chemistry

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