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rdf:type |
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lifeskim:mentions |
umls-concept:C0024579,
umls-concept:C0205464,
umls-concept:C0205531,
umls-concept:C0220781,
umls-concept:C0220825,
umls-concept:C0226896,
umls-concept:C0243077,
umls-concept:C0268563,
umls-concept:C0442027,
umls-concept:C0443288,
umls-concept:C0678594,
umls-concept:C0935763,
umls-concept:C1527415,
umls-concept:C1883254,
umls-concept:C2603343
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pubmed:issue |
17
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pubmed:dateCreated |
2006-7-25
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|
pubmed:abstractText |
Conformationally restricted 3-anilino-4-(3-indolyl)maleimide derivatives were designed and synthesized aiming at discovery of novel protein kinase Cbeta (PKCbeta)-selective inhibitors possessing oral bioavailability. Among them, compounds having a fused five-membered ring at the indole 1,2-position inhibited PKCbeta2 with IC50 of nM-order and showed good oral bioavailability. One of the most potent compounds was found to be PKCbeta-selective over other 6 isozymes and exhibited ameliorative effects in a rat diabetic retinopathy model via oral route.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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|
pubmed:status |
MEDLINE
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pubmed:month |
Sep
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pubmed:issn |
0968-0896
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|
pubmed:author |
pubmed-author:HaseYasunoriY,
pubmed-author:HoshiJun-ichiJ,
pubmed-author:IkemotoTomoyukiT,
pubmed-author:InabaTakashiT,
pubmed-author:MatsushitaMutsuyoshiM,
pubmed-author:SagawaShoichiS,
pubmed-author:SasaseTomohikoT,
pubmed-author:ShimomaFumitoF,
pubmed-author:TakahashiMitsuruM,
pubmed-author:TanakaMasahiroM,
pubmed-author:UbukataMinoruM,
pubmed-author:UedaNobuhisaN,
pubmed-author:YasueKatsutakaK
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|
pubmed:issnType |
Print
|
|
pubmed:day |
1
|
|
pubmed:volume |
14
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
5781-94
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|
pubmed:dateRevised |
2007-11-15
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|
pubmed:meshHeading |
pubmed-meshheading:16762554-Administration, Oral,
pubmed-meshheading:16762554-Animals,
pubmed-meshheading:16762554-Biological Availability,
pubmed-meshheading:16762554-Diabetes Mellitus, Experimental,
pubmed-meshheading:16762554-Diabetic Retinopathy,
pubmed-meshheading:16762554-Dose-Response Relationship, Drug,
pubmed-meshheading:16762554-Maleimides,
pubmed-meshheading:16762554-Molecular Structure,
pubmed-meshheading:16762554-Protein Kinase C,
pubmed-meshheading:16762554-Rats,
pubmed-meshheading:16762554-Structure-Activity Relationship
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|
pubmed:year |
2006
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|
pubmed:articleTitle |
Synthesis, SAR studies, and pharmacological evaluation of 3-anilino-4-(3-indolyl) maleimides with conformationally restricted structure as orally bioavailable PKCbeta-selective inhibitors.
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pubmed:affiliation |
Central Pharmaceutical Research Institute, Japan Tobacco Inc., Takatsuki Osaka 569-1125, Japan.
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pubmed:publicationType |
Journal Article
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