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dc.contributor.authorKamal, Ahmed
dc.contributor.authorSultana, Farheen
dc.contributor.authorRamaiah, M. Janaki
dc.contributor.authorSrikanth, Yellamelli V.V.
dc.contributor.authorViswanath, Arutla
dc.contributor.authorKishor, Chandan
dc.contributor.authorSharma, Pranjal
dc.contributor.authorPushpavalli, Sreerangam N.C.V.L.
dc.contributor.authorAddlagatta, Anthony
dc.contributor.authorPal-Bhadra, Manika
dc.date.accessioned2017-08-15T04:22:42Z
dc.date.available2017-08-15T04:22:42Z
dc.date.issued2012
dc.identifier.issn1860-7187
dc.identifier.doi10.1002/cmdc.201100511
dc.identifier.urihttp://hdl.handle.net/10072/344225
dc.description.abstractnew series of 3-substituted 2-phenylimidazo[2,1-b]benzothiazoles (3 a–h) were synthesized by C-arylation of 2-arylimidazo[2,1-b]benzothiazoles using palladium acetate as catalyst, and the resulting compounds were evaluated for their anticancer activity. Compounds 3 a, 3 e, and 3 h exhibited good antiproliferative activity, with GI50 values in the range of 0.19–83.1 μM. Compound 3 h showed potent anticancer efficacy against 60 human cancer cell lines, with a mean GI50 value of 0.88 μM. This compound also induced cell-cycle arrest in the G2/M phase and inhibited tubulin polymerization followed by activation of caspase-3 and apoptosis. A high-throughput tubulin polymerization assay showed that the level of inhibition for compound 3 h is similar to that of combretastatin A-4. Molecular modeling studies provided a molecular basis for the favorable binding of compounds 3 a, 3 e, and 3 h to the colchicine binding pocket of tubulin.
dc.description.peerreviewedYes
dc.languageEnglish
dc.language.isoeng
dc.publisherWiley
dc.relation.ispartofpagefrom292
dc.relation.ispartofpageto300
dc.relation.ispartofissue2
dc.relation.ispartofjournalChemMedChem
dc.relation.ispartofvolume7
dc.subject.fieldofresearchMedicinal and Biomolecular Chemistry not elsewhere classified
dc.subject.fieldofresearchMedicinal and Biomolecular Chemistry
dc.subject.fieldofresearchOrganic Chemistry
dc.subject.fieldofresearchPharmacology and Pharmaceutical Sciences
dc.subject.fieldofresearchcode030499
dc.subject.fieldofresearchcode0304
dc.subject.fieldofresearchcode0305
dc.subject.fieldofresearchcode1115
dc.title3-Substituted 2-Phenylimidazo[2,1-b]benzothiazoles: Synthesis, Anticancer Activity, and Inhibition of Tubulin Polymerization
dc.typeJournal article
dc.type.descriptionC1 - Articles
dc.type.codeC - Journal Articles
gro.hasfulltextNo Full Text
gro.griffith.authorKishor, Chandan


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