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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
8
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pubmed:dateCreated |
2011-4-4
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pubmed:abstractText |
We describe the design and synthesis of novel bicyclic spiro sulfonamides as potent Akt inhibitors. Through structure-based rational design, we have successfully improved PKA selectivity of previously disclosed spirochromanes. Representative compounds showed favorable Akt potency while exhibiting up to 1000-fold selectivity against PKA.
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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 |
Apr
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:BankaAnnaA,
pubmed-author:BencsikJosef RJR,
pubmed-author:BlakeJames FJF,
pubmed-author:BrandhuberBarbara JBJ,
pubmed-author:GloorSusan LSL,
pubmed-author:GrossStefan DSD,
pubmed-author:KallanNicholas CNC,
pubmed-author:MartinsonMatthewM,
pubmed-author:MitchellIan SIS,
pubmed-author:MoralesTony HTH,
pubmed-author:RisomTylerT,
pubmed-author:SkeltonNicholas JNJ,
pubmed-author:SpencerKeith LKL,
pubmed-author:TotBB,
pubmed-author:VigersGuy P AGP,
pubmed-author:WallaceEli MEM,
pubmed-author:WuWen-IWI
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pubmed:copyrightInfo |
Copyright © 2011 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 |
21
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2335-40
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pubmed:meshHeading |
pubmed-meshheading:21420856-Binding Sites,
pubmed-meshheading:21420856-Computer Simulation,
pubmed-meshheading:21420856-Crystallography, X-Ray,
pubmed-meshheading:21420856-Cyclic AMP-Dependent Protein Kinases,
pubmed-meshheading:21420856-Drug Evaluation, Preclinical,
pubmed-meshheading:21420856-Protein Kinase Inhibitors,
pubmed-meshheading:21420856-Proto-Oncogene Proteins c-akt,
pubmed-meshheading:21420856-Spiro Compounds,
pubmed-meshheading:21420856-Structure-Activity Relationship,
pubmed-meshheading:21420856-Sulfonamides
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pubmed:year |
2011
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pubmed:articleTitle |
Discovery of spirocyclic sulfonamides as potent Akt inhibitors with exquisite selectivity against PKA.
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pubmed:affiliation |
Array BioPharma Inc., 3200 Walnut Street, Boulder, CO 80301, USA. rxu@arraybiopharma.com
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pubmed:publicationType |
Journal Article
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