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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
14
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pubmed:dateCreated |
2009-7-13
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pubmed:abstractText |
Synthesis of novel 7-pseudo-steroids 1c has been achieved from trenbolone 3 via an efficient 14 step sequence with overall yields of 10-15%. Various substitutions were incorporated at both the aromatic side chain as well as the D ring. The orientation of aromatic side chain at C10 plays a crucial role for progesterone receptor (PR) activity. Compound 2a (T47D=1nM) with -NMe(2) para to the aromatic group along with spirofurane groups in the D ring was the optimal substitution. All compounds were also evaluated for glucocorticoid receptor (GR) antagonist activities in vivo in a rat and found efficacious in uterine complement C3 assay via the oral route of administrations.
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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 |
1464-3405
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pubmed:author |
pubmed-author:AllanGeorgeG,
pubmed-author:ChenXinX,
pubmed-author:DemarestKeithK,
pubmed-author:GunnetJosephJ,
pubmed-author:JainNareshkumarN,
pubmed-author:LintonOliviaO,
pubmed-author:LundeenScottS,
pubmed-author:MurrayWilliamW,
pubmed-author:QuM MMM,
pubmed-author:SuiZhihuaZ,
pubmed-author:TannenbaumPamelaP,
pubmed-author:ZhuPeifangP
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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 |
3977-80
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pubmed:dateRevised |
2011-11-17
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pubmed:meshHeading |
pubmed-meshheading:19217285-Administration, Oral,
pubmed-meshheading:19217285-Animals,
pubmed-meshheading:19217285-Benzoxepins,
pubmed-meshheading:19217285-Computer Simulation,
pubmed-meshheading:19217285-Crystallography, X-Ray,
pubmed-meshheading:19217285-Female,
pubmed-meshheading:19217285-Rats,
pubmed-meshheading:19217285-Rats, Sprague-Dawley,
pubmed-meshheading:19217285-Receptors, Glucocorticoid,
pubmed-meshheading:19217285-Receptors, Progesterone,
pubmed-meshheading:19217285-Structure-Activity Relationship,
pubmed-meshheading:19217285-Trenbolone Acetate
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pubmed:year |
2009
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pubmed:articleTitle |
Synthesis and SAR study of novel pseudo-steroids as potent and selective progesterone receptor antagonists.
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pubmed:affiliation |
Johnson and Johnson Pharmaceutical Research and Development, Medicinal Chemistry, LLC, Exton, PA 19341, USA. drnfjain@gmail.com
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pubmed:publicationType |
Journal Article
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