882977-67-5Relevant academic research and scientific papers
Synthesis and SAR of potent and selective androgen receptor antagonists: 5,6-Dichloro-benzimidazole derivatives
Ng, Raymond A.,Guan, Jihua,Alford Jr., Vernon C.,Lanter, James C.,Allan, George F.,Sbriscia, Tifanie,Linton, Olivia,Lundeen, Scott G.,Sui, Zhihua
, p. 784 - 788 (2007)
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).
