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Androstene-3,5-dienes as ER-beta selective SERMs.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2007 Nov 15; Vol. 17 (22), pp. 6295-8. Date of Electronic Publication: 2007 Sep 07. - Publication Year :
- 2007
-
Abstract
- A series of androstene-3,5-diene derivatives were prepared. Despite lacking the C-3 hydroxyl previously believed necessary for ER activity, some of the analogs retained surprising affinity for ER-beta. For example, diene 4 retained excellent selectivity and potency as an ER-beta agonist and was more selective for ER-beta over the androgen receptor (AR).
- Subjects :
- Androstadienes chemistry
Animals
Binding Sites drug effects
Crystallography, X-Ray
Humans
Inhibitory Concentration 50
Molecular Structure
Rats
Receptors, Androgen drug effects
Selective Estrogen Receptor Modulators chemistry
Androstadienes chemical synthesis
Androstadienes pharmacology
Estrogen Receptor beta agonists
Selective Estrogen Receptor Modulators chemical synthesis
Selective Estrogen Receptor Modulators pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 17
- Issue :
- 22
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 17890084
- Full Text :
- https://doi.org/10.1016/j.bmcl.2007.09.001