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

Gurupadaswamy, H. D. and Girish, V. and Kavitha, C. V. and Raghavan, S. C. and Khanum, S. A. (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 1768-3254

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Official URL: http://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
Uncontrolled Keywords: article, human, controlled study, drug screening, 1, 2, unclassified drug, drug synthesis, fluorouracil, 3, Dose-Response Relationship, Drug, Molecular Structure, 4 oxadiazole, 4 oxadiazole derivative, antineoplastic activity, cytotoxicity, Humans, Cell Line, Cell Survival, lactate dehydrogenase, Models, DNA fragmentation, Time Factors, antineoplastic agent, cell proliferation, Cell Proliferation, human cell, Tumor, Antineoplastic Agents, Antitumor, cancer inhibition, dose response, Drug Screening Assays, L-Lactate Dehydrogenase, apoptosis, cancer cell culture, cell survival, cell viability, Chemical, Inhibitory Concentration 50, Oxadiazoles, K562 Cells, 5 di(4 aryloylaryloxymethyl) 1, DNA Fragmentation, 5 di2 fluoro 4 (4 fluoro)benzoyl 6 chlorophenoxymethyl1, Intracellular Space
Subjects: C Chemical Science > Chemistry
Divisions: Yuvaraj college > Chemistry
Depositing User: Arshiya Kousar Library Assistant
Date Deposited: 13 Sep 2019 06:08
Last Modified: 13 Sep 2019 06:08
URI: http://eprints.uni-mysore.ac.in/id/eprint/8033

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