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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
5
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pubmed:dateCreated |
2008-3-10
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pubmed:abstractText |
A series of IGF-1R inhibitors is disclosed, wherein the (m-chlorophenyl)ethanol side chain of BMS-536924 (1) is replaced with a series of 2-(1H-imidazol-4-yl)ethanamine and 2-(1H-pyrazol-1-yl)ethanamine side chains. Some analogs show improved IGF-1R potency and oral exposure. Analogs from both series, 16a and 17f, show in vivo activity comparable to 1 in our constitutively activated IGF-1R Sal tumor model. This may be the due to the improved protein binding in human and mouse serum for imidazole 16a and the excellent oral exposure of pyrazole 17f.
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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 |
Mar
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:AttarRicardoR,
pubmed-author:BalimanePraveenP,
pubmed-author:CarboniJoanJ,
pubmed-author:EngGraceG,
pubmed-author:FrennessonDavid BDB,
pubmed-author:GottardisMarcoM,
pubmed-author:LangleyDavid RDR,
pubmed-author:LiAixinA,
pubmed-author:SangXiaopengX,
pubmed-author:SaulnierMark GMG,
pubmed-author:StruzynskiCharlesC,
pubmed-author:VelaparthiUpenderU,
pubmed-author:VyasDolatraiD,
pubmed-author:WittmanMark DMD,
pubmed-author:YangZhengZ,
pubmed-author:ZimmermannKurtK
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
18
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1702-7
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:18258427-Animals,
pubmed-meshheading:18258427-Antineoplastic Agents,
pubmed-meshheading:18258427-Benzimidazoles,
pubmed-meshheading:18258427-Humans,
pubmed-meshheading:18258427-Mice,
pubmed-meshheading:18258427-Molecular Structure,
pubmed-meshheading:18258427-Neoplasms, Experimental,
pubmed-meshheading:18258427-Protein Binding,
pubmed-meshheading:18258427-Pyridones,
pubmed-meshheading:18258427-Receptor, IGF Type 1,
pubmed-meshheading:18258427-Serum,
pubmed-meshheading:18258427-Structure-Activity Relationship
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pubmed:year |
2008
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pubmed:articleTitle |
2-(1H-Imidazol-4-yl)ethanamine and 2-(1H-pyrazol-1-yl)ethanamine side chain variants of the IGF-1R inhibitor BMS-536924.
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pubmed:affiliation |
Department of Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA. Mark.Saulnier@bms.com
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pubmed:publicationType |
Journal Article
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