Abstract
A series of novel 2-(1H-indol-2-yl)-propan-2-ols have been designed, synthesized, and screened for their ability to inhibit testosterone-induced prostate weight increases in immature rats. Through the use of this paradigm, we were able to identify compounds that exhibited in vivo potency equal to that of the marketed antiandrogen Casodex when orally administered.
MeSH terms
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Administration, Oral
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Androgen Antagonists / chemical synthesis
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Androgen Antagonists / chemistry*
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Androgen Antagonists / pharmacology*
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Androgen Receptor Antagonists*
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Anilides / pharmacology
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Animals
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Drug Evaluation, Preclinical / methods
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Indoles / chemical synthesis
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Indoles / chemistry*
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Indoles / pharmacology*
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Male
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Nitriles / pharmacology
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Prostate / drug effects*
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Rats
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Structure-Activity Relationship
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Tosyl Compounds / pharmacology
Substances
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Androgen Antagonists
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Androgen Receptor Antagonists
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Anilides
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Indoles
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Nitriles
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Tosyl Compounds
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bicalutamide