2-(2,2,2-Trifluoroethyl)-5,6-dichlorobenzimidazole derivatives as potent androgen receptor antagonists.
Publication/Presentation Date
2-15-2007
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).
Volume
17
Issue
4
First Page
955
Last Page
958
ISSN
0960-894X
Published In/Presented At
Ng, R. A., Guan, J., Alford, V. C., Jr, Lanter, J. C., Allan, G. F., Sbriscia, T., Lundeen, S. G., & Sui, Z. (2007). 2-(2,2,2-Trifluoroethyl)-5,6-dichlorobenzimidazole derivatives as potent androgen receptor antagonists. Bioorganic & medicinal chemistry letters, 17(4), 955–958. https://doi.org/10.1016/j.bmcl.2006.11.047
Disciplines
Education | Medical Education
PubMedID
17134895
Department(s)
Department of Education
Document Type
Article