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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
6
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pubmed:dateCreated |
2007-2-23
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pubmed:abstractText |
A series of selective androgen receptor modulators (SARMs) with a wide spectrum of receptor modulating activities was developed based on optimization of the 4-substituted 6-bisalkylamino-2-quinolinones (3). Significance of the trifluoromethyl group on the side chains and its interactions with amino acid residues within the androgen receptor (AR) ligand binding domain are discussed. A representative analog (9) was tested orally in a rodent model of hypogonadism and demonstrated desirable tissue selectivity.
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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 |
Mar
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:ChangWilliamW,
pubmed-author:KallelAdamA,
pubmed-author:LópezFrancisco JFJ,
pubmed-author:MarschkeKeith BKB,
pubmed-author:MartinboroughEstherE,
pubmed-author:MotamediMehrnoushM,
pubmed-author:Negro-VilarAndrésA,
pubmed-author:ShenYixingY,
pubmed-author:WestSarahS,
pubmed-author:ZhaoShuoS,
pubmed-author:ZhiLinL,
pubmed-author:van OeverenArjanA
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pubmed:issnType |
Print
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pubmed:day |
15
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pubmed:volume |
17
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1527-31
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:17267219-Androgen Antagonists,
pubmed-meshheading:17267219-Androgen Receptor Antagonists,
pubmed-meshheading:17267219-Androgens,
pubmed-meshheading:17267219-Animals,
pubmed-meshheading:17267219-Binding, Competitive,
pubmed-meshheading:17267219-Dihydrotestosterone,
pubmed-meshheading:17267219-Genitalia, Male,
pubmed-meshheading:17267219-Hypogonadism,
pubmed-meshheading:17267219-Indicators and Reagents,
pubmed-meshheading:17267219-Magnetic Resonance Spectroscopy,
pubmed-meshheading:17267219-Male,
pubmed-meshheading:17267219-Models, Molecular,
pubmed-meshheading:17267219-Molecular Conformation,
pubmed-meshheading:17267219-Orchiectomy,
pubmed-meshheading:17267219-Organ Size,
pubmed-meshheading:17267219-Organ Specificity,
pubmed-meshheading:17267219-Prostate,
pubmed-meshheading:17267219-Quinolines,
pubmed-meshheading:17267219-Rats,
pubmed-meshheading:17267219-Receptors, Androgen,
pubmed-meshheading:17267219-Structure-Activity Relationship,
pubmed-meshheading:17267219-Transfection
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pubmed:year |
2007
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pubmed:articleTitle |
Novel selective androgen receptor modulators: SAR studies on 6-bisalkylamino-2-quinolinones.
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pubmed:affiliation |
Discovery Research, Ligand Pharmaceuticals, 10275 Science Center Drive, San Diego, CA 92121, USA.
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pubmed:publicationType |
Journal Article
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