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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
16
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pubmed:dateCreated |
2009-7-29
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pubmed:abstractText |
We have designed and synthesized a novel series of pyrrolidinones as progesterone receptor partial agonists. Compounds from this series had improved AR selectivity, rat pharmacokinetic properties, and in vivo potency compared to the lead compound. In addition, these compounds had improved selectivity against hERG channel inhibition.
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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 |
Aug
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:BrayJeffrey DJD,
pubmed-author:DuraiswamiChayaC,
pubmed-author:FrazeeJames SJS,
pubmed-author:GlaceLindsay ELE,
pubmed-author:GrygielkoEugene TET,
pubmed-author:HammondMarlysM,
pubmed-author:HoangTram HTH,
pubmed-author:JohnsonLatishaL,
pubmed-author:MadaussKevin PKP,
pubmed-author:MannsSharadaS,
pubmed-author:NagillaRakeshR,
pubmed-author:StewartEugene LEL,
pubmed-author:ThompsonScott KSK,
pubmed-author:TranThuy BTB,
pubmed-author:TriznaWalterW,
pubmed-author:WashburnDavid GDG,
pubmed-author:WilliamsShawn PSP
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
19
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4664-8
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pubmed:meshHeading |
pubmed-meshheading:19616429-Administration, Oral,
pubmed-meshheading:19616429-Animals,
pubmed-meshheading:19616429-Binding Sites,
pubmed-meshheading:19616429-Drug Discovery,
pubmed-meshheading:19616429-Ether-A-Go-Go Potassium Channels,
pubmed-meshheading:19616429-Haplorhini,
pubmed-meshheading:19616429-Humans,
pubmed-meshheading:19616429-Pyrrolidinones,
pubmed-meshheading:19616429-Rats,
pubmed-meshheading:19616429-Receptors, Progesterone,
pubmed-meshheading:19616429-Structure-Activity Relationship
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pubmed:year |
2009
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pubmed:articleTitle |
Discovery of orally active, pyrrolidinone-based progesterone receptor partial agonists.
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pubmed:affiliation |
Department of Chemistry, Metabolic Pathways Centre for Excellence in Drug Discovery, GlaxoSmithKline Pharmaceuticals, King of Prussia, PA 19406, USA. dave.g.washburn@gsk.com
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pubmed:publicationType |
Journal Article
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