Source:http://linkedlifedata.com/resource/pubmed/id/11859003
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
5
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pubmed:dateCreated |
2002-2-22
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pubmed:abstractText |
Novel 6-aryl benzoxazines were prepared and examined as progesterone receptor (PR) modulators. In contrast to the structurally related 6-aryl dihydroquinoline PR antagonists, the 6-aryl benzoxazines were potent PR agonists. Compounds 4e, 5b, and 6a with the 2,4,4-trimethyl-1,4-dihydro-2H-benzo[d][1,3]oxazine core were the most potent PR agonists in the series with sub-nanomolar activities (EC(50) 0.20-0.35nM). Compound 6a was more potent than progesterone (P4) in the in vivo decidualization assay in an ovariectomized female rat model by subcutaneous administration with an ED(50) of 1.5mg/kg (vs 5.62mg/kg for P4).
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Mar
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pubmed:issn |
0960-894X
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
11
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pubmed:volume |
12
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
787-90
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pubmed:dateRevised |
2003-11-14
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pubmed:meshHeading |
pubmed-meshheading:11859003-Animals,
pubmed-meshheading:11859003-Female,
pubmed-meshheading:11859003-Injections, Subcutaneous,
pubmed-meshheading:11859003-Models, Animal,
pubmed-meshheading:11859003-Molecular Structure,
pubmed-meshheading:11859003-Ovariectomy,
pubmed-meshheading:11859003-Oxazines,
pubmed-meshheading:11859003-Rats,
pubmed-meshheading:11859003-Receptors, Progesterone,
pubmed-meshheading:11859003-Structure-Activity Relationship
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pubmed:year |
2002
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pubmed:articleTitle |
Potent nonsteroidal progesterone receptor agonists: synthesis and SAR study of 6-aryl benzoxazines.
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pubmed:affiliation |
Medicinal Chemistry I, Chemical Sciences, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, USA. zhangp@war.wyeth.com
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pubmed:publicationType |
Journal Article
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