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Estrogen receptor ligands. Part 11: Synthesis and activity of isochromans and isothiochromans.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2005 Feb 01; Vol. 15 (3), pp. 715-8. - Publication Year :
- 2005
-
Abstract
- The ring oxygen and sulfur analogs of lasofoxifene, 1a and 1b, were synthesized in an attempt to impart ERalpha selectivity, as found in the closely related dihydrobenzoxathiin compound I, recently discovered in these laboratories. The resulting isochroman and isothiochroman compounds were found to exhibit equipotent binding affinities to the ER isoforms and were less active in the inhibition of estradiol-triggered uterine growth when compared to I and lasofoxifene.
- Subjects :
- Cell Line, Tumor
Cell Proliferation drug effects
Estradiol pharmacology
Female
Humans
Inhibitory Concentration 50
Ligands
Models, Molecular
Protein Binding
Protein Isoforms
Structure-Activity Relationship
Uterus drug effects
Uterus growth & development
Chromans chemical synthesis
Chromans pharmacology
Estrogen Receptor alpha metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 15
- Issue :
- 3
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 15664843
- Full Text :
- https://doi.org/10.1016/j.bmcl.2004.11.018