Source:http://linkedlifedata.com/resource/pubmed/id/19524602
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
12
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pubmed:dateCreated |
2009-9-14
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pubmed:abstractText |
Inhibition of aromatase is an efficient approach for the prevention and treatment of breast cancer. New 6beta,19-bridged steroid analogs of androstenedione, 6beta,19-epithio- and 6beta,19-methano compounds 11 and 17, were synthesized starting from 19-hydroxyandrostenedione (6) and 19-formylandrost-5-ene-3beta,17beta-yl diacetate (12), respectively, as aromatase inhibitors. All of the compounds including known steroids 6beta,19-epoxyandrostenedione (4) and 6beta,19-cycloandrostenedione (5) tested were weak to poor competitive inhibitors of aromatase and, among them, 6beta,19-epoxy steroid 4 provided only moderate inhibition (K(i): 2.2 microM). These results show that the 6beta,19-bridged groups of the inhibitors interfere with binding in active site of aromatase.
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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 |
Nov
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pubmed:issn |
1878-5867
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pubmed:author | |
pubmed:issnType |
Electronic
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pubmed:volume |
74
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
884-9
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pubmed:meshHeading |
pubmed-meshheading:19524602-Androstenedione,
pubmed-meshheading:19524602-Aromatase,
pubmed-meshheading:19524602-Aromatase Inhibitors,
pubmed-meshheading:19524602-Female,
pubmed-meshheading:19524602-Humans,
pubmed-meshheading:19524602-Inhibitory Concentration 50,
pubmed-meshheading:19524602-Placenta,
pubmed-meshheading:19524602-Pregnancy
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pubmed:year |
2009
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pubmed:articleTitle |
6beta,19-Bridged androstenedione analogs as aromatase inhibitors.
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pubmed:affiliation |
Tohoku Pharmaceutical University, 4-1 Komatsushima-4-chome, Aoba-ku, Sendai 981-8558, Japan.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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