Author/Authors :
Raymond A. Ng، نويسنده , , Jihua Guan، نويسنده , , Vernon C. Alford Jr.، نويسنده , , James C. Lanter، نويسنده , , George F. Allan، نويسنده , , Tifanie Sbriscia، نويسنده , , Olivia Linton، نويسنده , , Scott G. Lundeen، نويسنده , , Zhihua Sui، نويسنده ,
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).
