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dc.contributor.authorKamal, Ahmed
dc.contributor.authorShaik, Anver Basha
dc.contributor.authorJain, Nishant
dc.contributor.authorKishor, Chandan
dc.contributor.authorNagabhushana, Ananthamurthy
dc.contributor.authorSupriya, Bhukya
dc.contributor.authorKumar, G. Bharath
dc.contributor.authorChourasiya, Sumit S.
dc.contributor.authorSuresh, Yerramsetty
dc.contributor.authorMishra, Rakesh K.
dc.contributor.authorAddlagatta, Anthony
dc.date.accessioned2017-08-14T01:37:14Z
dc.date.available2017-08-14T01:37:14Z
dc.date.issued2015
dc.identifier.issn0223-5234
dc.identifier.doi10.1016/j.ejmech.2013.10.077
dc.identifier.urihttp://hdl.handle.net/10072/343953
dc.description.abstractA series of twenty one compounds with pyrazole and oxindole conjugates were synthesized by Knoevenagel condensation and investigated for their antiproliferative activity on different human cancer cell lines. The conjugates are comprised of a four ring scaffold; the structural isomers 12b and 12c possess chloro-substitution in the D ring. Among the congeners 12b, 12c, and 12d manifested significant cytotoxicity and inhibited tubulin assembly. Treatments with 12b, 12c and 12d resulted in accumulation of cells in G2/M phase, disruption of microtubule network, and increase in cyclin B1 protein. Zebrafish screening revealed that 12b, and 12d caused developmental defects. Docking analysis demonstrated that the congeners occupy the colchicine binding pocket of tubulin.
dc.description.peerreviewedYes
dc.languageEnglish
dc.language.isoeng
dc.publisherElsevier
dc.relation.ispartofpagefrom501
dc.relation.ispartofpageto513
dc.relation.ispartofjournalEuropean Journal of Medicinal Chemistry
dc.relation.ispartofvolume92
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.titleDesign and synthesis of pyrazole-oxindole conjugates targeting tubulin polymerization as new anticancer agents
dc.typeJournal article
dc.type.descriptionC1 - Articles
dc.type.codeC - Journal Articles
gro.hasfulltextNo Full Text
gro.griffith.authorKishor, Chandan


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