dc.contributor.author | Kamal, Ahmed | |
dc.contributor.author | Sultana, Farheen | |
dc.contributor.author | Ramaiah, M. Janaki | |
dc.contributor.author | Srikanth, Yellamelli V.V. | |
dc.contributor.author | Viswanath, Arutla | |
dc.contributor.author | Kishor, Chandan | |
dc.contributor.author | Sharma, Pranjal | |
dc.contributor.author | Pushpavalli, Sreerangam N.C.V.L. | |
dc.contributor.author | Addlagatta, Anthony | |
dc.contributor.author | Pal-Bhadra, Manika | |
dc.date.accessioned | 2017-08-15T04:22:42Z | |
dc.date.available | 2017-08-15T04:22:42Z | |
dc.date.issued | 2012 | |
dc.identifier.issn | 1860-7187 | |
dc.identifier.doi | 10.1002/cmdc.201100511 | |
dc.identifier.uri | http://hdl.handle.net/10072/344225 | |
dc.description.abstract | new 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.peerreviewed | Yes | |
dc.language | English | |
dc.language.iso | eng | |
dc.publisher | Wiley | |
dc.relation.ispartofpagefrom | 292 | |
dc.relation.ispartofpageto | 300 | |
dc.relation.ispartofissue | 2 | |
dc.relation.ispartofjournal | ChemMedChem | |
dc.relation.ispartofvolume | 7 | |
dc.subject.fieldofresearch | Medicinal and Biomolecular Chemistry not elsewhere classified | |
dc.subject.fieldofresearch | Medicinal and Biomolecular Chemistry | |
dc.subject.fieldofresearch | Organic Chemistry | |
dc.subject.fieldofresearch | Pharmacology and Pharmaceutical Sciences | |
dc.subject.fieldofresearchcode | 030499 | |
dc.subject.fieldofresearchcode | 0304 | |
dc.subject.fieldofresearchcode | 0305 | |
dc.subject.fieldofresearchcode | 1115 | |
dc.title | 3-Substituted 2-Phenylimidazo[2,1-b]benzothiazoles: Synthesis, Anticancer Activity, and Inhibition of Tubulin Polymerization | |
dc.type | Journal article | |
dc.type.description | C1 - Articles | |
dc.type.code | C - Journal Articles | |
gro.hasfulltext | No Full Text | |
gro.griffith.author | Kishor, Chandan | |