Synthesis of potent and tissue-selective androgen receptor modulators (SARMs): 2-(2,2,2)-Trifluoroethyl-benzimidazole scaffold.
Publication/Presentation Date
3-15-2007
Abstract
The synthesis and in vivo SAR of 2-(2,2,2)-trifluoroethyl-benzimidazoles are described. Prostate antagonism and/or levator ani agonism can be modulated by varying the substitution at the 2-position of 5,6-dichloro-benzimidazoles. Potent androgen agonists on the muscle were discovered that strongly bind to the androgen receptor (2-17 nM) and show potent in vivo efficacy (0.03-0.11 mg/day). True SARMs showing both prostate antagonism and levator ani agonism were revealed.
Volume
17
Issue
6
First Page
1784
Last Page
1787
ISSN
0960-894X
Published In/Presented At
Ng, R. A., Lanter, J. C., Alford, V. C., Allan, G. F., Sbriscia, T., Lundeen, S. G., & Sui, Z. (2007). Synthesis of potent and tissue-selective androgen receptor modulators (SARMs): 2-(2,2,2)-Trifluoroethyl-benzimidazole scaffold. Bioorganic & medicinal chemistry letters, 17(6), 1784–1787. https://doi.org/10.1016/j.bmcl.2006.12.045
Disciplines
Education | Medical Education
PubMedID
17197181
Department(s)
Department of Education
Document Type
Article