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dc.contributor.authorKamal, Ahmed
dc.contributor.authorViswanath, Arutla
dc.contributor.authorRamaiah, M. Janaki
dc.contributor.authorMurty, J. NSRC
dc.contributor.authorSultana, Farheen
dc.contributor.authorRamakrishna, Gajula
dc.contributor.authorTamboli, Jaki R.
dc.contributor.authorPushpavalli, Sreerangam N.C.V.L.
dc.contributor.authorPal, Dhananjaya
dc.contributor.authorKishor, Chandan
dc.contributor.authorAddlagatta, Anthony
dc.contributor.authorBhadra, Manika P.
dc.date.accessioned2017-10-05T00:01:15Z
dc.date.available2017-10-05T00:01:15Z
dc.date.issued2012
dc.identifier.issn2040-2503
dc.identifier.doi10.1039/c2md20085f
dc.identifier.urihttp://hdl.handle.net/10072/347865
dc.description.abstractA new series of tetrazole based isoxazolines (4a–l) was synthesized and evaluated for their anticancer potential against two cancer cell lines. All these compounds exhibited profound cytotoxicity with IC50 values ranging from 1.22 to 3.62 μM and compounds 4h, 4i showed prominent anticancer efficacy with IC50 values of 1.51, 1.49 μM in A549 and 2.83, 2.40 μM in MDA-MB-231 cell lines. Further, these compounds (4h, 4i) induced apoptotic cell death by inhibition of tubulin polymerization leading to cell cycle arrest at G2/M phase of the cell cycle followed by caspase-3 activity. Moreover, the level of tubulin inhibition by these compounds was examined by in vitro HTS tubulin polymerization assay. Docking of compound 4h and 4i to the active site of tubulin revealed that the trimethoxy ring of the compounds occupies the colchicine binding site of tubulin, whereas the isoxazoline moiety moves towards the interface of α–β tubulin and involves a series of hydrogen bonds with αTyr224 and αSer178.
dc.description.peerreviewedYes
dc.languageEnglish
dc.language.isoeng
dc.publisherRSC Publications
dc.relation.ispartofpagefrom1386
dc.relation.ispartofpageto1392
dc.relation.ispartofissue11
dc.relation.ispartofjournalMedChemComm
dc.relation.ispartofvolume3
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.titleSynthesis of tetrazole-isoxazoline hybrids as a new class of tubulin polymerization inhibitors
dc.typeJournal article
dc.type.descriptionC1 - Articles
dc.type.codeC - Journal Articles
gro.hasfulltextNo Full Text
gro.griffith.authorKishor, Chandan


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