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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
9
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pubmed:dateCreated |
2011-4-25
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pubmed:abstractText |
Human murine double minute 2 (MDM2) is a negative regulator of p53, which plays an important role in cell cycle and apoptosis. We report several optimizations to the synthesis of the chromenotriazolopyrimidine series of MDM2-p53 protein-protein interaction inhibitors. Additionally, the in vitro and in vivo stability, pharmacokinetic properties and solubility were improved through N-substitution.
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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 |
May
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:AllenJohn GJG,
pubmed-author:BeckHilary PHP,
pubmed-author:DeGraffenreidMichaelM,
pubmed-author:FoxBrianB,
pubmed-author:OlinerJonathan DJD,
pubmed-author:OlsonStevenS,
pubmed-author:RewYosupY,
pubmed-author:SaikiAnne YAY,
pubmed-author:SalyersKevinK,
pubmed-author:SchneiderStephenS,
pubmed-author:YeQiupingQ,
pubmed-author:YuDongyinD
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pubmed:copyrightInfo |
Copyright © 2010 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
1
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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 |
2752-5
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pubmed:meshHeading |
pubmed-meshheading:21123063-Animals,
pubmed-meshheading:21123063-Drug Stability,
pubmed-meshheading:21123063-Humans,
pubmed-meshheading:21123063-Infusion Pumps,
pubmed-meshheading:21123063-Inhibitory Concentration 50,
pubmed-meshheading:21123063-Molecular Structure,
pubmed-meshheading:21123063-Proto-Oncogene Proteins c-mdm2,
pubmed-meshheading:21123063-Pyrimidines,
pubmed-meshheading:21123063-Rats,
pubmed-meshheading:21123063-Solubility,
pubmed-meshheading:21123063-Structure-Activity Relationship,
pubmed-meshheading:21123063-Tumor Suppressor Protein p53
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pubmed:year |
2011
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pubmed:articleTitle |
Improvement of the synthesis and pharmacokinetic properties of chromenotriazolopyrimidine MDM2-p53 protein-protein inhibitors.
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pubmed:affiliation |
Chemistry Research & Discovery, Amgen Inc., 1120 Veterans Blvd, South San Francisco, CA 94080, USA. hbeck@amgen.com
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pubmed:publicationType |
Journal Article
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