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dc.contributor.authorPooja, R K-
dc.contributor.authorJoseph, M M-
dc.contributor.authorAbdul Salam, A A-
dc.contributor.authorSreelekha, T T-
dc.contributor.authorDhanya, S-
dc.contributor.authorBiswas, S-
dc.contributor.authorPai, K S R-
dc.date.accessioned2018-07-10T05:59:05Z-
dc.date.available2018-07-10T05:59:05Z-
dc.date.issued2017-11-
dc.identifier.citationJournal of Biochemical and Molecular Toxicology, 31(11):e21962en_US
dc.identifier.urihttp://10.10.100.66:8080/xmlui/handle/123456789/3173-
dc.description.abstractIn the pursuit of novel anticancer leads, new bisindole-oxadiazoles were synthesized using propyl phosphonic anhydride as a mild and efficient reagent. The molecule, 3-[5-(1H-indol-3-ylmethyl)- 1,3,4-oxadiazol-2-yl]-1H-indole (3a) exhibited selective cytotoxicity to MCF-7 cells with a cell cycle arrest in the G1 phase. The mechanism of cytotoxicity of 3a involved caspase-2-dependent apoptotic pathway with characteristic apoptoticmorphological alterations as observed in acridine orange/ethidium bromide and Hoechst staining. The wound healing migratory assay exhibited an intense impairment in themotility ofMCF-7 cells on incubationwith 3a.Docking simulations with anti-apoptotic protein Bcl-2, which is also involved in cancer metastasis displayed good affinity and high binding energy of 3a into the well characterized BH3 binding site. The positive correlation between the Bcl-2 binding studies and the results of in vitro investigations exemplifies compound 3a as a lead molecule exhibiting MCF-7 differential cytotoxicity via apoptotic mode of cell death in addition to its anti-metastatic activity.en_US
dc.language.isoenen_US
dc.publisherWileyen_US
dc.subjectapoptosisen_US
dc.subjectbisindole-oxadiazoleen_US
dc.subjectBcl-2en_US
dc.subjectcaspasesen_US
dc.subjectmigrationen_US
dc.titleBisindole-Oxadiazole Hybrids, T3P®-Mediated Synthesis, and Appraisal of Their Apoptotic, Antimetastatic, and Computational Bcl-2 Binding Potentialen_US
dc.typeArticleen_US
Appears in Collections:2017

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