Synthesis of potent and tissue-selective androgen receptor modulators (SARMs): 2-(2,2,2)-Trifluoroethyl-benzimidazole scaffold

The synthesis and in vivo SAR of 2-(2,2,2)-trifluoroethyl-benzimidazoles are described. Prostate antagonism and/or levator ani agonism can be modulated by varying the substitution at the 2-position of 5,6-dichloro-benzimidazoles. Potent androgen agonists on the muscle were discovered that strongly b...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2007-03, Vol.17 (6), p.1784-1787
Hauptverfasser:	Ng, Raymond A., Lanter, James C., Alford, Vernon C., Allan, George F., Sbriscia, Tifanie, Lundeen, Scott G., Sui, Zhihua
Format:	Artikel
Sprache:	eng
Schlagworte:	Androgen Receptor Antagonists Androgens Animals Benzimidazoles Benzimidazoles - agonists Benzimidazoles - antagonists & inhibitors Benzimidazoles - chemical synthesis Biological and medical sciences Dose-Response Relationship, Drug Hormones. Endocrine system In vivo screening Indicators and Reagents Male Medical sciences Models, Molecular Muscle, Smooth - drug effects Muscle, Smooth - metabolism Organ Size - drug effects Pharmacology. Drug treatments Prostate - drug effects Prostate - metabolism Rats Rats, Sprague-Dawley Receptors, Androgen - drug effects SARM Structure-Activity Relationship
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