Synthesis and SAR of potent and selective androgen receptor antagonists: 5,6-Dichloro-benzimidazole derivatives.
Publication/Presentation Date
2-1-2007
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).
Volume
17
Issue
3
First Page
784
Last Page
788
ISSN
0960-894X
Published In/Presented At
Ng, R. A., Guan, J., Alford, V. C., Jr, Lanter, J. C., Allan, G. F., Sbriscia, T., Linton, O., Lundeen, S. G., & Sui, Z. (2007). Synthesis and SAR of potent and selective androgen receptor antagonists: 5,6-Dichloro-benzimidazole derivatives. Bioorganic & medicinal chemistry letters, 17(3), 784–788. https://doi.org/10.1016/j.bmcl.2006.10.071
Disciplines
Education | Medical Education
PubMedID
17095226
Department(s)
Department of Education
Document Type
Article