2-(2,2,2-Trifluoroethyl)-5,6-dichlorobenzimidazole derivatives as potent androgen receptor antagonists

The synthesis and in vivo SAR of N-benzyl, N-aceto, and N-ethylene ether derivatives of 2-(2,2,2-trifluoroethyl)-5,6-dichloro-benzimidazole as novel androgen receptor antagonists are described. SAR studies led to the discovery of 4-bromo-benzyl benzimidazole 17 as a more potent androgen receptor ant...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2007-02, Vol.17 (4), p.955-958
Hauptverfasser:	Ng, Raymond A., Guan, Jihua, Alford, Vernon C., Lanter, James C., Allan, George F., Sbriscia, Tifanie, Lundeen, Scott G., Sui, Zhihua
Format:	Artikel
Sprache:	eng
Schlagworte:	Alkylation Androgen Antagonists - chemical synthesis Androgen Antagonists - pharmacology Androgen Receptor Antagonists Anilides - pharmacology Animals Antineoplastic agents Antineoplastic Agents, Hormonal - chemical synthesis Antineoplastic Agents, Hormonal - pharmacology Benzimidazoles Benzimidazoles - chemical synthesis Benzimidazoles - pharmacology Bicalutamide Biological and medical sciences General aspects Indicators and Reagents Male Medical sciences Nitriles - pharmacology Orchiectomy Organ Size - drug effects Pharmacology. Drug treatments Prostate - drug effects Rats Rats, Sprague-Dawley Structure-Activity Relationship Tosyl Compounds - pharmacology
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Zusammenfassung:	The synthesis and in vivo SAR of N-benzyl, N-aceto, and N-ethylene ether derivatives of 2-(2,2,2-trifluoroethyl)-5,6-dichloro-benzimidazole as novel androgen receptor antagonists are described. SAR studies led to the discovery of 4-bromo-benzyl benzimidazole 17 as a more potent androgen receptor antagonist in the rat prostate (ID 50 = 0.13 mg/day), compared with bicalutamide (ID 50 = 0.23 mg/day).
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2006.11.047