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  • Title: 2-(2,2,2-Trifluoroethyl)-5,6-dichlorobenzimidazole derivatives as potent androgen receptor antagonists.
    Author: Ng RA, Guan J, Alford VC, Lanter JC, Allan GF, Sbriscia T, Lundeen SG, Sui Z.
    Journal: Bioorg Med Chem Lett; 2007 Feb 15; 17(4):955-8. PubMed ID: 17134895.
    Abstract:
    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)=0.13mg/day), compared with bicalutamide (ID(50)=0.23mg/day).
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