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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
20
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pubmed:dateCreated |
2008-10-20
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pubmed:abstractText |
A series of 4-amino-6-benzimidazole-pyrimidines was designed to target lymphocyte-specific tyrosine kinase (Lck), a member of the Src kinase family. Highly efficient parallel syntheses were devised to prepare analogues for SAR studies. A number of these 4-amino-6-benzimidazole-pyrimidines exhibited single-digit nanomolar IC(50)s against Lck in biochemical and cellular assays. These 4-amino-6-benzimidazole-pyrimidines represent a new class of tyrosine kinase inhibitors.
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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 |
Oct
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:CheJianweiJ,
pubmed-author:ChowDonaldD,
pubmed-author:GrayNathanael SNS,
pubmed-author:HeYunY,
pubmed-author:IskandarMayaM,
pubmed-author:KaranewskyDonald SDS,
pubmed-author:LiuYiY,
pubmed-author:Martin SeidelHH,
pubmed-author:RenPingdaP,
pubmed-author:RomeoRussellR,
pubmed-author:SandbergMark LML,
pubmed-author:SimTaeboT,
pubmed-author:SpaldingTracy ATA,
pubmed-author:TianShin-ShaySS,
pubmed-author:WangXiaX,
pubmed-author:ZhangGuobaoG
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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 |
5618-21
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:18793846-Autoimmune Diseases,
pubmed-meshheading:18793846-Benzimidazoles,
pubmed-meshheading:18793846-Chemistry, Pharmaceutical,
pubmed-meshheading:18793846-Drug Design,
pubmed-meshheading:18793846-Humans,
pubmed-meshheading:18793846-Inhibitory Concentration 50,
pubmed-meshheading:18793846-Lymphocyte Specific Protein Tyrosine Kinase p56(lck),
pubmed-meshheading:18793846-Models, Chemical,
pubmed-meshheading:18793846-Molecular Conformation,
pubmed-meshheading:18793846-Protein-Tyrosine Kinases,
pubmed-meshheading:18793846-Pyrimidines,
pubmed-meshheading:18793846-Solubility,
pubmed-meshheading:18793846-Structure-Activity Relationship,
pubmed-meshheading:18793846-src-Family Kinases
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pubmed:year |
2008
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pubmed:articleTitle |
Discovery of pyrimidine benzimidazoles as Lck inhibitors: part I.
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pubmed:affiliation |
Genomics Institute of the Novartis Research Foundation (GNF), Medicinal Chemistry, 10715 John Jay Hopkins Drive, San Diego, CA 92121, USA. gzhang@gnf.org
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pubmed:publicationType |
Journal Article
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