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Abstract
We report herein the synthesis, characterization, and cytotoxicity evaluations of some newer oxadiazole and triazole analogues (5a-j). The cytotoxicity of all the title compounds were evaluated as per the National Cancer Institute protocol in a one-dose assay (10 $\mu $M) on nine different panels of 59 cancer cell lines. 2-$\{$5-[(2,4-Dichlorophenoxy)methyl]-1,3,4-oxadiazol-2-yl$\}$phenol (5e) showed the maximum cytotoxicity among the series of ten compounds. The cytotoxicity of 5e was comparable to that of the standard anticancer drug, 5-fluorouracil, and better than that of imatinib. The structure activity relationship was also discussed.
Highlights
Cancer is uncontrolled growth of abnormal cells that grow outside their usual boundaries and assault the adjoining parts of the body and spread to other organs
2 There are many types of cancer treatment, and the treatment strategy depends upon cancer type and stage
3 Chemotherapy is a major part of cancer therapeutics; it has its own limitations of limited efficacy, selectivity, high cost, genotoxicity, and drug resistance
Summary
Cancer is uncontrolled growth of abnormal cells that grow outside their usual boundaries and assault the adjoining parts of the body and spread to other organs. 3 Chemotherapy is a major part of cancer therapeutics; it has its own limitations of limited efficacy, selectivity, high cost, genotoxicity, and drug resistance. Compounds containing heterocyclic rings are of great importance both in medicine and industry. Oxadiazoles have a large impact on multiple drug discovery programs across a variety of therapeutic areas, including tuberculosis, 6 cancer, 7 HIV, 8 diabetes, 9 obesity, inflammation, and infection. The carbonyl compounds of amides, ester, carbamates, and hydroxamic acids have been successfully replaced with oxadiazole rings for improved efficacy. 13−15 triazole analogues are well reported anticancer agents. 16,17 The literature on oxadizoles and our previous published work 18 is a source of inspiration to continue research on further exploration of oxadiazole, and in the present investigation we report the synthesis and cytotoxicity evaluation of some new oxadiazole analogues.
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