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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
13
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pubmed:dateCreated |
2008-6-16
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pubmed:abstractText |
Novel 7-aryl benzo[1,4]oxazepin-2-ones were synthesized and evaluated as non-steroidal progesterone receptor (PR) modulators. The structure activity relationship of 7-aryl benzo[1,4]oxazepinones was examined using the T47D cell alkaline phosphatase assay. A number of 7-aryl benzo[1,4]oxazepinones such as 10j and 10v demonstrated good in vitro potency (IC(50) of 10-30 nM) and selectivity (over 100-fold) at PR over other steroidal receptors such as glucocorticoid and androgen receptors (GR and AR). Several 7-aryl benzo[1,4]oxazepinones were active in the rat uterine decidualization model. In this in vivo model, compounds 10j and 10u were active at 3 mg/kg when dosed orally.
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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 |
Jul
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pubmed:issn |
1464-3391
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pubmed:author |
pubmed-author:BerrodinThomas JTJ,
pubmed-author:CohenJeffreyJ,
pubmed-author:FensomeAndrewA,
pubmed-author:KernJeffrey CJC,
pubmed-author:TerefenkoEugene AEA,
pubmed-author:UnwallaRayR,
pubmed-author:WinnekerRichard CRC,
pubmed-author:WrobelJayJ,
pubmed-author:YudtMatthew RMR,
pubmed-author:ZhangPuwenP,
pubmed-author:ZhangZhimingZ
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
16
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
6589-600
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pubmed:meshHeading |
pubmed-meshheading:18504132-Alkaline Phosphatase,
pubmed-meshheading:18504132-Animals,
pubmed-meshheading:18504132-Benzazepines,
pubmed-meshheading:18504132-Binding Sites,
pubmed-meshheading:18504132-COS Cells,
pubmed-meshheading:18504132-Cercopithecus aethiops,
pubmed-meshheading:18504132-Female,
pubmed-meshheading:18504132-Hydroxylation,
pubmed-meshheading:18504132-Models, Molecular,
pubmed-meshheading:18504132-Molecular Structure,
pubmed-meshheading:18504132-Oxazepines,
pubmed-meshheading:18504132-Receptors, Progesterone,
pubmed-meshheading:18504132-Structure-Activity Relationship
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pubmed:year |
2008
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pubmed:articleTitle |
7-aryl 1,5-dihydro-benzo[e][1,4]oxazepin-2-ones and analogs as non-steroidal progesterone receptor antagonists.
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pubmed:affiliation |
Chemical and Screening Sciences, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, USA. Zhangp@wyeth.com
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pubmed:publicationType |
Journal Article
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