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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
24
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pubmed:dateCreated |
2008-11-25
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pubmed:abstractText |
A new series of pyrazolo[3,4-d]pyrimidine-3,6-diamines was designed and synthesized as potent and selective inhibitors of the nonreceptor tyrosine kinase, ACK1. These compounds arose from efforts to rigidify an earlier series of N-aryl pyrimidine-5-carboxamides. The synthesis and structure-activity relationships of this new series of inhibitors are reported. The most promising compounds were also profiled for their pharmacokinetic properties.
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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 |
Dec
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:CardozoMario GMG,
pubmed-author:FarrellyEllynE,
pubmed-author:FengZ LZL,
pubmed-author:FuJiashengJ,
pubmed-author:HaoXiaolinX,
pubmed-author:JaenJuan CJC,
pubmed-author:JiaoXianYunX,
pubmed-author:KayserFrankF,
pubmed-author:KopeckyDavid JDJ,
pubmed-author:LiShyunS,
pubmed-author:LiuJinsongJ,
pubmed-author:WalkerNigel P CNP,
pubmed-author:WangZhulunZ,
pubmed-author:WescheHolgerH,
pubmed-author:XiaoShou-HuaSH
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pubmed:issnType |
Electronic
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pubmed:day |
15
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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 |
6352-6
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pubmed:dateRevised |
2011-7-1
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pubmed:meshHeading |
pubmed-meshheading:18993068-Animals,
pubmed-meshheading:18993068-Chemistry, Pharmaceutical,
pubmed-meshheading:18993068-Crystallography, X-Ray,
pubmed-meshheading:18993068-Diamines,
pubmed-meshheading:18993068-Drug Design,
pubmed-meshheading:18993068-Enzyme Inhibitors,
pubmed-meshheading:18993068-Inhibitory Concentration 50,
pubmed-meshheading:18993068-Male,
pubmed-meshheading:18993068-Models, Chemical,
pubmed-meshheading:18993068-Molecular Conformation,
pubmed-meshheading:18993068-Protein-Tyrosine Kinases,
pubmed-meshheading:18993068-Pyrazoles,
pubmed-meshheading:18993068-Pyrimidines,
pubmed-meshheading:18993068-Rats,
pubmed-meshheading:18993068-Rats, Sprague-Dawley,
pubmed-meshheading:18993068-Structure-Activity Relationship
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pubmed:year |
2008
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pubmed:articleTitle |
Identification and optimization of N3,N6-diaryl-1H-pyrazolo[3,4-d]pyrimidine-3,6-diamines as a novel class of ACK1 inhibitors.
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pubmed:affiliation |
Department of Chemistry, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA. dkopecky@amgen.com
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pubmed:publicationType |
Journal Article
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