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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
2
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pubmed:dateCreated |
2010-2-3
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pubmed:abstractText |
The synthesis and evaluation of tetrasubstituted aminopyridines, bearing novel azaindazole hinge binders, as potent AKT inhibitors are described. Compound 14c was identified as a potent AKT inhibitor that demonstrated reduced CYP450 inhibition and an improved developability profile compared to those of previously described trisubstituted pyridines. It also displayed dose-dependent inhibition of both phosphorylation of GSK3beta and tumor growth in a BT474 tumor xenograft model in mice.
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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 |
Jan
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:BrownBarry SBS,
pubmed-author:BrownKristin KKK,
pubmed-author:ChoudhryAnthony EAE,
pubmed-author:DonovanBrian TBT,
pubmed-author:HeerdingDirk ADA,
pubmed-author:JulMM,
pubmed-author:KahanaJason AJA,
pubmed-author:KumarRakeshR,
pubmed-author:LafranceLouisL,
pubmed-author:LaiZhihongZ,
pubmed-author:LeberJackJ,
pubmed-author:LevyDanaD,
pubmed-author:LinHongH,
pubmed-author:LuengoJuan IJI,
pubmed-author:MinthornElisabeth AEA,
pubmed-author:RobellKimberly AKA,
pubmed-author:SafonovIgor GIG,
pubmed-author:SchaberMichaelM,
pubmed-author:TakataDennisD,
pubmed-author:VenslavskyJosephJ,
pubmed-author:VermaSharadS,
pubmed-author:WangWenyongW,
pubmed-author:XieRenR,
pubmed-author:YamashitaDennis SDS,
pubmed-author:ZengJinJ,
pubmed-author:ZhangShuyunS
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pubmed:copyrightInfo |
Copyright 2009 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
20
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
684-8
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pubmed:dateRevised |
2011-11-2
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pubmed:meshHeading |
pubmed-meshheading:20006500-Aminopyridines,
pubmed-meshheading:20006500-Animals,
pubmed-meshheading:20006500-Cell Line, Tumor,
pubmed-meshheading:20006500-Cytochrome P-450 Enzyme System,
pubmed-meshheading:20006500-Dogs,
pubmed-meshheading:20006500-Ether-A-Go-Go Potassium Channels,
pubmed-meshheading:20006500-Glycogen Synthase Kinase 3,
pubmed-meshheading:20006500-Haplorhini,
pubmed-meshheading:20006500-Humans,
pubmed-meshheading:20006500-Mice,
pubmed-meshheading:20006500-Phosphorylation,
pubmed-meshheading:20006500-Protein Kinase Inhibitors,
pubmed-meshheading:20006500-Proto-Oncogene Proteins c-akt,
pubmed-meshheading:20006500-Pyrazines,
pubmed-meshheading:20006500-Pyridines,
pubmed-meshheading:20006500-Rats,
pubmed-meshheading:20006500-Structure-Activity Relationship,
pubmed-meshheading:20006500-Xenograft Model Antitumor Assays
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pubmed:year |
2010
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pubmed:articleTitle |
Tetrasubstituted pyridines as potent and selective AKT inhibitors: Reduced CYP450 and hERG inhibition of aminopyridines.
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pubmed:affiliation |
Oncology Medicinal Chemistry, GlaxoSmithKline, 1250 S. Collegeville Rd., Collegeville, PA 19426, United States. hong.2.lin@gsk.com
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pubmed:publicationType |
Journal Article
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