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Please use this identifier to cite or link to this item: http://dspace.bits-pilani.ac.in:8080/jspui/handle/123456789/15519
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dc.contributor.authorKumar, Anil-
dc.contributor.authorKumar, Dalip-
dc.date.accessioned2024-09-11T04:00:57Z-
dc.date.available2024-09-11T04:00:57Z-
dc.date.issued2021-04-
dc.identifier.urihttps://www.sciencedirect.com/science/article/pii/S0960894X21000688-
dc.identifier.urihttp://dspace.bits-pilani.ac.in:8080/jspui/xmlui/handle/123456789/15519-
dc.description.abstractA series of novel indolyl-α-keto-1,3,4-oxadiazole derivatives have been synthesized by employing molecular iodine-mediated oxidative cyclization of acylhydrazones. In vitro anti cell proliferation activity of these derivatives against various cancer cells lines such as human lymphoblast (U937), leukemia (Jurkat & SB) and human breast (BT474) was investigated. Among the synthesized indolyl-α-keto-1,3,4-oxadiazoles 19a-p, only one compound (19e) exhibited significant antiproliferative activity against a panel of cell lines. The compound 19e with 3,4,5-trimethoxyphenyl motif, endowed strong cytotoxicity against U937, Jurkat, BT474 and SB cancer cells with IC50 values of 7.1, 3.1, 4.1, and 0.8 µM, respectively. Molecular docking studies suggested a potential binding mode for 19e in the colchicine binding site of tubulin. When tested for in vitro tubulin polymerizaton, 19e inhibited tubulin polymezations (IC50 = 10.66 µM) and induced apoptosis through caspase 3/7 activation. Further, the derivative 19e did not cause necrosis when measured using lactate dehydrogenase assay.en_US
dc.language.isoenen_US
dc.publisherElsevieren_US
dc.subjectChemistryen_US
dc.subjectIndolyl-α-keto-1,3,4-oxadiazolesen_US
dc.subjectCytotoxicityen_US
dc.subjectApoptosisen_US
dc.subjectTubulin inhibitoren_US
dc.titleIndolyl-α-keto-1,3,4-oxadiazoles: Synthesis, anti-cell proliferation activity, and inhibition of tubulin polymerizationen_US
dc.typeArticleen_US
Appears in Collections:Department of Chemistry

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