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

…, GF Allan, T Sbriscia, O Linton, SG Lundeen…

Index: Ng, Raymond A.; Guan, Jihua; Alford Jr., Vernon C.; Lanter, James C.; Allan, George F.; Sbriscia, Tifanie; Linton, Olivia; Lundeen, Scott G.; Sui, Zhihua Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 3 p. 784 - 788

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Citation Number: 26

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).