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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
7
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pubmed:dateCreated |
2009-4-2
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pubmed:abstractText |
The design and synthesis of a novel series of oxazole-, thiazole-, and imidazole-based inhibitors of IkappaB kinase (IKK) are reported. Biological activity was improved compared to the pyrazolopurine lead, and the expedient synthesis of the new tricyclic systems allowed for efficient exploration of structure-activity relationships. This, combined with an iterative rat cassette dosing strategy, was used to identify compounds with improved pharmacokinetic (PK) profiles to advance for in vivo evaluation.
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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 |
http://linkedlifedata.com/resource/pubmed/chemical/Glutathione Transferase,
http://linkedlifedata.com/resource/pubmed/chemical/Heterocyclic Compounds, 3-Ring,
http://linkedlifedata.com/resource/pubmed/chemical/I-kappa B Kinase,
http://linkedlifedata.com/resource/pubmed/chemical/Imidazoles,
http://linkedlifedata.com/resource/pubmed/chemical/Lipopolysaccharides,
http://linkedlifedata.com/resource/pubmed/chemical/Oxazoles,
http://linkedlifedata.com/resource/pubmed/chemical/Recombinant Fusion Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/TNF protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Thiazoles,
http://linkedlifedata.com/resource/pubmed/chemical/Tumor Necrosis Factor-alpha
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pubmed:status |
MEDLINE
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pubmed:month |
Apr
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pubmed:issn |
1520-4804
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pubmed:author |
pubmed-author:BarrishJoel CJC,
pubmed-author:BelangerDominiqueD,
pubmed-author:BurkeJames RJR,
pubmed-author:ChenLaishunL,
pubmed-author:DasJagabandhuJ,
pubmed-author:DoddJohn HJH,
pubmed-author:DodierMarcoM,
pubmed-author:DyckmanAlaric JAJ,
pubmed-author:FurchJoseph AJA,
pubmed-author:GillPatriceP,
pubmed-author:GilloolyKathleenK,
pubmed-author:GuoJunqingJ,
pubmed-author:KempsonJamesJ,
pubmed-author:LangevineCharles MCM,
pubmed-author:LiTianleT,
pubmed-author:MarathePunit HPH,
pubmed-author:MarinierAnneA,
pubmed-author:MartelAlainA,
pubmed-author:McIntyreKim WKW,
pubmed-author:McKinnonMurrayM,
pubmed-author:MoquinRobert VRV,
pubmed-author:NirschlDavidD,
pubmed-author:PattoliMark AMA,
pubmed-author:PittsWilliam JWJ,
pubmed-author:QuesnelleClaudeC,
pubmed-author:SpergelSteven HSH,
pubmed-author:Van KirkKatyK,
pubmed-author:Wang-IversonDavidD,
pubmed-author:WattersonScott HSH,
pubmed-author:YangZhengZ
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pubmed:issnType |
Electronic
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pubmed:day |
9
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pubmed:volume |
52
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1994-2005
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:19267461-Animals,
pubmed-meshheading:19267461-Crystallography, X-Ray,
pubmed-meshheading:19267461-Female,
pubmed-meshheading:19267461-Glutathione Transferase,
pubmed-meshheading:19267461-Heterocyclic Compounds, 3-Ring,
pubmed-meshheading:19267461-Humans,
pubmed-meshheading:19267461-I-kappa B Kinase,
pubmed-meshheading:19267461-Imidazoles,
pubmed-meshheading:19267461-Leukocytes, Mononuclear,
pubmed-meshheading:19267461-Lipopolysaccharides,
pubmed-meshheading:19267461-Mice,
pubmed-meshheading:19267461-Mice, Inbred BALB C,
pubmed-meshheading:19267461-Microsomes, Liver,
pubmed-meshheading:19267461-Oxazoles,
pubmed-meshheading:19267461-Rats,
pubmed-meshheading:19267461-Recombinant Fusion Proteins,
pubmed-meshheading:19267461-Structure-Activity Relationship,
pubmed-meshheading:19267461-Thiazoles,
pubmed-meshheading:19267461-Tumor Necrosis Factor-alpha
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pubmed:year |
2009
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pubmed:articleTitle |
Novel tricyclic inhibitors of IkappaB kinase.
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pubmed:affiliation |
Departments of Discovery Chemistry, Discovery Biology, and Metabolism and Pharmacokinetics and Synthesis and Analysis Technology Team, Bristol-Myers Squibb Research and Development, Princeton, New Jersey 08543-4000, USA.
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pubmed:publicationType |
Journal Article,
In Vitro
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