Linked Life Data

14980636

Source:http://linkedlifedata.com/resource/pubmed/id/14980636

Statements in which the resource exists.
SubjectPredicateObjectContext
pubmed-article:14980636rdf:typepubmed:Citationlld:pubmed
pubmed-article:14980636lifeskim:mentionsumls-concept:C0330390lld:lifeskim
pubmed-article:14980636lifeskim:mentionsumls-concept:C0017932lld:lifeskim
pubmed-article:14980636lifeskim:mentionsumls-concept:C0244989lld:lifeskim
pubmed-article:14980636lifeskim:mentionsumls-concept:C0220781lld:lifeskim
pubmed-article:14980636lifeskim:mentionsumls-concept:C0220825lld:lifeskim
pubmed-article:14980636lifeskim:mentionsumls-concept:C1883254lld:lifeskim
pubmed-article:14980636lifeskim:mentionsumls-concept:C0243077lld:lifeskim
pubmed-article:14980636lifeskim:mentionsumls-concept:C0205250lld:lifeskim
pubmed-article:14980636lifeskim:mentionsumls-concept:C0679622lld:lifeskim
pubmed-article:14980636lifeskim:mentionsumls-concept:C0205314lld:lifeskim
pubmed-article:14980636lifeskim:mentionsumls-concept:C0205460lld:lifeskim
pubmed-article:14980636pubmed:issue5lld:pubmed
pubmed-article:14980636pubmed:dateCreated2004-2-24lld:pubmed
pubmed-article:14980636pubmed:abstractTextPalladium catalyzed cross-coupling reactions were used to synthesize two key intermediates 3 and 5 that resulted in the synthesis of novel series of macrocyclic bis-7-azaindolylmaleimides. Among the three series of macrocycles, the oxygen atom and thiophene containing linkers yielded molecules with higher inhibitory potency at GSK-3 beta (K(i)=0.011-0.079 microM) while the nitrogen atom containing linkers yielded molecules with lower potency (K(i)=0.150->1 microM). Compound 33 and 36 displayed 1-2 orders of magnitude selectivity at GSK-3 beta against CDK2, PKC beta II, Rsk3 and little or no inhibitions to the other 62 protein kinases. Compound 46 was at least 100-fold more selective towards GSK-3 beta than PKC beta II, and it had little or no activity against a panel of 65 protein kinases, almost behaved as a GSK-3 beta 'specific inhibitor'. All three compounds showed good potency in GS assay. Molecular docking studies were conducted in an attempt to rationalize the GSK-3 beta selectivity of azaindolylmaleimides. The high selectivity, inhibitory potency and cellular activities of these non-crown-ether typed molecules may provide them as a valuable pharmacological tools in elucidating the complex roles of GSK-3 beta in cell signaling pathways and the potential usage for the treatment of elevated level of GSK-3 beta involved diseases.lld:pubmed
pubmed-article:14980636pubmed:languageenglld:pubmed
pubmed-article:14980636pubmed:journalhttp://linkedlifedata.com/r...lld:pubmed
pubmed-article:14980636pubmed:citationSubsetIMlld:pubmed
pubmed-article:14980636pubmed:chemicalhttp://linkedlifedata.com/r...lld:pubmed
pubmed-article:14980636pubmed:chemicalhttp://linkedlifedata.com/r...lld:pubmed
pubmed-article:14980636pubmed:chemicalhttp://linkedlifedata.com/r...lld:pubmed
pubmed-article:14980636pubmed:chemicalhttp://linkedlifedata.com/r...lld:pubmed
pubmed-article:14980636pubmed:chemicalhttp://linkedlifedata.com/r...lld:pubmed
pubmed-article:14980636pubmed:statusMEDLINElld:pubmed
pubmed-article:14980636pubmed:monthMarlld:pubmed
pubmed-article:14980636pubmed:issn0968-0896lld:pubmed
pubmed-article:14980636pubmed:authorpubmed-author:ChenXinXlld:pubmed
pubmed-article:14980636pubmed:authorpubmed-author:ShenLanLlld:pubmed
pubmed-article:14980636pubmed:authorpubmed-author:BeaversMary...lld:pubmed
pubmed-article:14980636pubmed:authorpubmed-author:MurrayWilliam...lld:pubmed
pubmed-article:14980636pubmed:authorpubmed-author:KuoGee-HongGHlld:pubmed
pubmed-article:14980636pubmed:authorpubmed-author:DemarestKeith...lld:pubmed
pubmed-article:14980636pubmed:authorpubmed-author:ConwayBruce...lld:pubmed
pubmed-article:14980636pubmed:authorpubmed-author:XuJun ZJZlld:pubmed
pubmed-article:14980636pubmed:authorpubmed-author:WestoverLoriLlld:pubmed
pubmed-article:14980636pubmed:authorpubmed-author:ProutyCatheri...lld:pubmed
pubmed-article:14980636pubmed:authorpubmed-author:LookRichard...lld:pubmed
pubmed-article:14980636pubmed:authorpubmed-author:RobertsJerryJlld:pubmed
pubmed-article:14980636pubmed:issnTypePrintlld:pubmed
pubmed-article:14980636pubmed:day1lld:pubmed
pubmed-article:14980636pubmed:volume12lld:pubmed
pubmed-article:14980636pubmed:ownerNLMlld:pubmed
pubmed-article:14980636pubmed:authorsCompleteYlld:pubmed
pubmed-article:14980636pubmed:pagination1239-55lld:pubmed
pubmed-article:14980636pubmed:dateRevised2011-11-2lld:pubmed
pubmed-article:14980636pubmed:meshHeadingpubmed-meshheading:14980636...lld:pubmed
pubmed-article:14980636pubmed:meshHeadingpubmed-meshheading:14980636...lld:pubmed
pubmed-article:14980636pubmed:meshHeadingpubmed-meshheading:14980636...lld:pubmed
pubmed-article:14980636pubmed:meshHeadingpubmed-meshheading:14980636...lld:pubmed
pubmed-article:14980636pubmed:meshHeadingpubmed-meshheading:14980636...lld:pubmed
pubmed-article:14980636pubmed:meshHeadingpubmed-meshheading:14980636...lld:pubmed
pubmed-article:14980636pubmed:meshHeadingpubmed-meshheading:14980636...lld:pubmed
pubmed-article:14980636pubmed:meshHeadingpubmed-meshheading:14980636...lld:pubmed
pubmed-article:14980636pubmed:meshHeadingpubmed-meshheading:14980636...lld:pubmed
pubmed-article:14980636pubmed:meshHeadingpubmed-meshheading:14980636...lld:pubmed
pubmed-article:14980636pubmed:year2004lld:pubmed
pubmed-article:14980636pubmed:articleTitleSynthesis and biological evaluation of novel macrocyclic bis-7-azaindolylmaleimides as potent and highly selective glycogen synthase kinase-3 beta (GSK-3 beta) inhibitors.lld:pubmed
pubmed-article:14980636pubmed:affiliationDrug Discovery Division, Johnson and Johnson Pharmaceutical Research and Development, L.L.C., 1000 Route 202, PO Box 300, Raritan, NJ 08869, USA.lld:pubmed
pubmed-article:14980636pubmed:publicationTypeJournal Articlelld:pubmed
http://linkedlifedata.com/r...pubmed:referesTopubmed-article:14980636lld:pubmed