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DC Field | Value | Language |
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dc.contributor.author | Kumar, Dalip | - |
dc.date.accessioned | 2021-10-27T04:20:51Z | - |
dc.date.available | 2021-10-27T04:20:51Z | - |
dc.date.issued | 2011-07 | - |
dc.identifier.uri | https://www.sciencedirect.com/science/article/pii/S0223523411002455?via%3Dihub | - |
dc.identifier.uri | http://dspace.bits-pilani.ac.in:8080/xmlui/handle/123456789/3051 | - |
dc.description.abstract | A library of 3,5-disubstituted-1,2,4-oxadiazoles 7–9 and their bioisosters, 1,3,4-oxadiazole 14 and 1,3,4-thiadiazole 16, were synthesized and evaluated in vitro for their anticancer potential against a panel of six human cancer cell lines. The key step in the synthesis of oxadiazoles 7–9 involve coupling of amidoxime 6 with an appropriate carboxylic acid followed by thermal cyclization. The bioisosteres, 1,3,4-oxadiazole 14 and 1,3,4-thiadiazole 16 were prepared from the reaction of a common precursor diacylhydrazine 13 with thionyl chloride and Lawesson′s reagent, respectively. The anticancer studies on the synthesized compounds revealed that presence of a cyclopentyloxy or n-butyloxy on the C-3 aryl ring and piperdin-4-yl or trichloromethyl at the C-5 position of 1,2,4-oxadiazole is essential for good activity. In particular, 1,2,4-oxadiazole 7i and analogue 1,3,4-thiadiazole 16 exhibited significant activity against DU145 (IC50: 9.3 μM) and MDA-MB-231 (IC50: 9.2 μM) cell lines, respectively. | en_US |
dc.language.iso | en | en_US |
dc.publisher | Elsiever | en_US |
dc.subject | Chemistry | en_US |
dc.subject | 1,2,4-Oxadiazole | en_US |
dc.subject | 1,3,4-Thiadiazoles | en_US |
dc.subject | Anticancer agents | en_US |
dc.title | Synthesis of novel 1,2,4-oxadiazoles and analogues as potential anticancer agents | en_US |
dc.type | Article | en_US |
Appears in Collections: | Department of Chemistry |
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