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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
3
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pubmed:dateCreated |
2002-3-7
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pubmed:abstractText |
Synthesis and SARs of new integrin alpha(V)beta(3) antagonists based on an N-substituted dibenzazepinone scaffold are described. Variation of spacer and guanidine mimetic led to potent compounds exhibiting an IC(50) towards alpha(V)beta(3) in the nanomolar range, high selectivity versus integrin alpha(IIb)beta(3) and efficacy in functional cellular assays.
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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 |
Feb
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:BackfischGiselaG,
pubmed-author:DelzerJürgenJ,
pubmed-author:GenesteHervéH,
pubmed-author:GraefClaudiaC,
pubmed-author:HolzenkampUtaU,
pubmed-author:HornbergerWilfriedW,
pubmed-author:KlingAndreasA,
pubmed-author:LangeUdo E WUE,
pubmed-author:LauterbachArnulfA,
pubmed-author:MackHelmutH,
pubmed-author:SeitzWernerW,
pubmed-author:SubkowskiThomasT
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pubmed:issnType |
Print
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pubmed:day |
11
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pubmed:volume |
12
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
441-6
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:11814816-Dibenzazepines,
pubmed-meshheading:11814816-Drug Design,
pubmed-meshheading:11814816-Drug Evaluation, Preclinical,
pubmed-meshheading:11814816-Fibrinolytic Agents,
pubmed-meshheading:11814816-Guanidine,
pubmed-meshheading:11814816-Indicators and Reagents,
pubmed-meshheading:11814816-Mass Spectrometry,
pubmed-meshheading:11814816-Platelet Glycoprotein GPIIb-IIIa Complex,
pubmed-meshheading:11814816-Receptors, Vitronectin,
pubmed-meshheading:11814816-Structure-Activity Relationship
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pubmed:year |
2002
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pubmed:articleTitle |
Synthesis and SAR of N-substituted dibenzazepinone derivatives as novel potent and selective alpha(V)beta(3) antagonists.
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pubmed:affiliation |
Knoll GmbH, D-67008 Ludwigshafen, Germany. andreas.kling@abbott.de
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pubmed:publicationType |
Journal Article
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