Abstract
The androgen receptor is a member of the extended family of nuclear receptors and is widely distributed throughout the body. Androgen therapy is used to compensate for low levels of the natural hormones testosterone (T) and dihydrotestosterone and consists of administration of T, prodrugs thereof, or synthetic androgens. However, currently available androgens have many drawbacks. We identified 6-dialkylamino-4-trifluoromethylquinolin-2(1H)-ones as orally available tissue-selective androgen receptor modulators.
MeSH terms
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Administration, Oral
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Aminoquinolines / chemical synthesis*
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Aminoquinolines / chemistry
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Aminoquinolines / pharmacology
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Androgens / chemical synthesis*
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Androgens / chemistry
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Androgens / pharmacology
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Animals
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Binding Sites
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Binding, Competitive
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Humans
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In Vitro Techniques
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Male
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Models, Molecular
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Orchiectomy
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Organ Size
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Pelvic Floor / anatomy & histology
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Prostate / anatomy & histology
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Prostate / drug effects
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Quinolines / chemical synthesis*
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Quinolines / chemistry
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Quinolines / pharmacology
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Quinolones / chemical synthesis*
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Quinolones / chemistry
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Quinolones / pharmacology
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Rats
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Receptors, Androgen / drug effects*
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Receptors, Androgen / metabolism
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Structure-Activity Relationship
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Transfection
Substances
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6-N,N-bis(2,2,2-trifluoroethyl)amino-4-trifluoromethylquinolin-2(1H)-one
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Aminoquinolines
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Androgens
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Quinolines
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Quinolones
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Receptors, Androgen