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DC Field | Value | Language |
---|---|---|
dc.contributor.author | Kumar, Anil | - |
dc.date.accessioned | 2021-10-14T13:09:29Z | - |
dc.date.available | 2021-10-14T13:09:29Z | - |
dc.date.issued | 2021-02-05 | - |
dc.identifier.uri | https://europepmc.org/article/med/33556575 | - |
dc.identifier.uri | http://dspace.bits-pilani.ac.in:8080/xmlui/handle/123456789/2807 | - |
dc.description.abstract | A 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.iso | en | en_US |
dc.publisher | PMC | en_US |
dc.subject | Chemistry | en_US |
dc.subject | Polymerization | en_US |
dc.subject | Synthesis | en_US |
dc.subject | Anti-cell proliferation activity | en_US |
dc.title | Indolyl-α-keto-1,3,4-oxadiazoles: Synthesis, anti-cell proliferation activity, and inhibition of tubulin polymerization | en_US |
dc.type | Article | en_US |
Appears in Collections: | Department of Chemistry |
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