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dc.contributor.authorEl-Deeb, Ibrahim Mustafa
dc.contributor.authorLee, So
dc.date.accessioned2017-05-03T15:59:05Z
dc.date.available2017-05-03T15:59:05Z
dc.date.issued2010
dc.date.modified2011-07-19T06:25:42Z
dc.identifier.issn09680896
dc.identifier.doi10.1016/j.bmc.2010.04.037
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.
dc.description.peerreviewedYes
dc.description.publicationstatusYes
dc.languageEnglish
dc.language.isoeng
dc.publisherElsevier
dc.publisher.placeUnited Kingdom
dc.relation.ispartofstudentpublicationN
dc.relation.ispartofpagefrom3860
dc.relation.ispartofpageto3874
dc.relation.ispartofissue11
dc.relation.ispartofjournalBioorganic & Medicinal Chemistry
dc.relation.ispartofvolume18
dc.rights.retentionY
dc.subject.fieldofresearchBiologically Active Molecules
dc.subject.fieldofresearchMedicinal and Biomolecular Chemistry
dc.subject.fieldofresearchOrganic Chemistry
dc.subject.fieldofresearchPharmacology and Pharmaceutical Sciences
dc.subject.fieldofresearchcode030401
dc.subject.fieldofresearchcode0304
dc.subject.fieldofresearchcode0305
dc.subject.fieldofresearchcode1115
dc.titleDesign and Synthesis of New Anticancer Pyrimidines with Multiple-kinase Inhibitory Effect
dc.typeJournal article
dc.type.descriptionC1 - Articles
dc.type.codeC - Journal Articles
gro.date.issued2010
gro.hasfulltextNo Full Text
gro.griffith.authorEl-Deeb, Ibrahim Mustafa


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