Back to Search
Start Over
Estrogen receptor ligands. Part 4: The SAR of the syn-dihydrobenzoxathiin SERAMs.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2004 Jun 07; Vol. 14 (11), pp. 2741-5. - Publication Year :
- 2004
-
Abstract
- A series of estrogen receptor ligands based on a dihydrobenzoxathiin scaffold is described and evaluated for estrogen/anti-estrogen activity in both in vitro and in vivo models. The most active analogue, 22, was found to be 40-fold ERalpha selective in a competitive binding assay, and 22 demonstrated very potent in vivo antagonism of estradiol driven proliferation in an immature rat uterine weight gain assay.
- Subjects :
- Animals
Binding, Competitive
Cell Line, Tumor
Cell Proliferation drug effects
Estrogen Receptor beta chemistry
Female
Heterocyclic Compounds, 4 or More Rings chemical synthesis
Heterocyclic Compounds, 4 or More Rings pharmacokinetics
Heterocyclic Compounds, 4 or More Rings pharmacology
Humans
Ligands
Organ Size
Oxathiins chemical synthesis
Oxathiins pharmacokinetics
Protein Binding
Rats
Rats, Sprague-Dawley
Selective Estrogen Receptor Modulators pharmacokinetics
Selective Estrogen Receptor Modulators pharmacology
Structure-Activity Relationship
Uterus drug effects
Estrogen Receptor alpha chemistry
Oxathiins pharmacology
Selective Estrogen Receptor Modulators chemical synthesis
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 14
- Issue :
- 11
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 15125925
- Full Text :
- https://doi.org/10.1016/j.bmcl.2004.03.074