R. Ng, J. Guan, V. Alford
Feb 1, 2007
Citations
0
Influential Citations
34
Citations
Journal
Bioorganic & medicinal chemistry letters
Abstract
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 (ID50 = 0.15 mg/day).