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dc.contributor.authorEl-Deeb, Ibrahim Mustafaen_US
dc.contributor.authorLee, Soen_US
dc.date.accessioned2017-04-24T13:35:45Z
dc.date.available2017-04-24T13:35:45Z
dc.date.issued2010en_US
dc.date.modified2011-07-19T06:25:42Z
dc.identifier.issn09680896en_US
dc.identifier.doi10.1016/j.bmc.2010.04.037en_AU
dc.identifier.urihttp://hdl.handle.net/10072/37819
dc.description.abstractA new series of N-substituted-2-aminopyrimidines based on the '4-(pyridin-3-yl)pyrimidin-2-amine' scaffold of Imatinib has been designed and synthesized. A selected group from the target compounds was tested over a panel of 60 cancer cell lines at a single dose concentration of 10 卬 and the two most active compounds, 25b and 30, were further tested in a five-dose testing mode to determine their IC50 values over the 60 cell lines. Compound 30 has showed good potencies and high efficacies, and was accordingly tested at a single dose concentration of 10 占over a panel of 54 kinases. At this concentration, the compound has showed multiple inhibitions over a number of oncogenic kinases, including ABL1, AKT1, LCK, C-SRC, PIM1, FLT3, FYN, and KDR. A molecular modeling study was made by docking of the most active compound 30 and its inactive analog 29 into the kinase domain of ABL1 to investigate their possible binding interactions.en_US
dc.description.peerreviewedYesen_US
dc.description.publicationstatusYesen_AU
dc.languageEnglishen_US
dc.language.isoen_AU
dc.publisherElsevieren_US
dc.publisher.placeUnited Kingdomen_US
dc.relation.ispartofstudentpublicationNen_AU
dc.relation.ispartofpagefrom3860en_US
dc.relation.ispartofpageto3874en_US
dc.relation.ispartofissue11en_US
dc.relation.ispartofjournalBioorganic & Medicinal Chemistryen_US
dc.relation.ispartofvolume18en_US
dc.rights.retentionYen_AU
dc.subject.fieldofresearchBiologically Active Moleculesen_US
dc.subject.fieldofresearchcode030401en_US
dc.titleDesign and Synthesis of New Anticancer Pyrimidines with Multiple-kinase Inhibitory Effecten_US
dc.typeJournal articleen_US
dc.type.descriptionC1 - Peer Reviewed (HERDC)en_US
dc.type.codeC - Journal Articlesen_US
gro.date.issued2010
gro.hasfulltextNo Full Text


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