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dc.contributor.authorSuman, Pathi
dc.contributor.authorMurthy, T. Ramalinga
dc.contributor.authorRajkumar, Kommera
dc.contributor.authorSrikanth, Dudem
dc.contributor.authorDayakar, Cherupally
dc.contributor.authorKishor, Chandan
dc.contributor.authorAddlagatta, Anthony
dc.contributor.authorKalivendi, Shasi V.
dc.contributor.authorRaju, Bhimapaka C.
dc.date.accessioned2017-08-14T12:31:15Z
dc.date.available2017-08-14T12:31:15Z
dc.date.issued2015
dc.identifier.issn0223-5234
dc.identifier.doi10.1016/j.ejmech.2014.11.063
dc.identifier.urihttp://hdl.handle.net/10072/343952
dc.description.abstractThree series of compounds; pyridinyl-1H-1,2,3-triazoles, pyridinyl-1H-1,2,3-triazolylisoxazoles and pyridinyl-1H-1,2,3-triazolyldihydroisoxazoles with TMP moiety were designed, synthesized and screened for their anti-cancer and anti-tubulin properties. By sequentially designing three series of compounds comprising of dihydroisoxazole in the linker, a small substituent like chlorine on one side (R1) and aromatic group (R) on the pyridine ring, we have optimized the anti-cancer as well as anti-tubulin activity. Pyridinyl-1H-1,2,3-triazolyldihydroisoxazoles 28b and 28c were found to be potent anti-cancer agents against all the cell lines tested with a concomitant accumulation of cells in the G2/M phase of the cell cycle. Molecular modeling suggests that the trimethoxyphenyl ring in 28b and 28c occupies the cholchicine binding domain of β-tubulin, whereas, the dihydroisoxazole extends towards the interface of α,β-tubulin.
dc.description.peerreviewedYes
dc.languageEnglish
dc.language.isoeng
dc.publisherElsevier
dc.relation.ispartofpagefrom603
dc.relation.ispartofpageto619
dc.relation.ispartofjournalEuropean Journal of Medicinal Chemistry
dc.relation.ispartofvolume90
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 and structure-activity relationships of pyridinyl-1H -1,2,3-triazolyldihydroisoxazoles as potent inhibitors 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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