Synthesis and SAR of potent and selective androgen receptor antagonists: 5,6-Dichloro-benzimidazole derivatives

The synthesis and in vivo SAR of 5,6-dichloro-benzimidazole derivatives as novel selective androgen receptor antagonists are described. During screening of 2-alkyl benzimidazoles, it was found that a trifluoromethyl group greatly enhances antagonist activity in the prostate. Benzimidazole 1 is a pot...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2007-02, Vol.17 (3), p.784-788
Hauptverfasser:	Ng, Raymond A., Guan, Jihua, Alford, Vernon C., Lanter, James C., Allan, George F., Sbriscia, Tifanie, Linton, Olivia, Lundeen, Scott G., Sui, Zhihua
Format:	Artikel
Sprache:	eng
Schlagworte:	Androgen Antagonists - chemical synthesis Androgen Antagonists - pharmacology Androgen Receptor Antagonists Animals Benzimidazoles Benzimidazoles - chemical synthesis Benzimidazoles - pharmacology Indicators and Reagents Male Molecular Weight Orchiectomy Prostate - drug effects Prostate weight Rats Rats, Sprague-Dawley Structure-Activity Relationship Sulfides - chemical synthesis Sulfones - chemical synthesis
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Zusammenfassung:	The synthesis and in vivo SAR of 5,6-dichloro-benzimidazole derivatives as novel selective androgen receptor antagonists are described. During screening of 2-alkyl benzimidazoles, it was found that a trifluoromethyl group greatly enhances antagonist activity in the prostate. Benzimidazole 1 is a potent AR antagonist in the rat prostate (ID 50 = 0.15 mg/day).
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2006.10.071