Synthesis and estrogenic activities of novel 7-thiosubstituted estratriene derivatives.
A diastereomerically pure series of 7alpha-thioestratrienes was prepared and evaluated for its affinity for both the human estrogen receptor alpha and the more recently discovered estrogen receptor beta. The functional estrogenic activities of the compounds were measured in a MCF-7 ERE-tk-luciferase assay. The activities and selectivities of the compounds were sensitive to the nature of the thioether side chain.
Miller
C P
CP
Chemical Sciences, Wyeth-Ayerst Research, Radnor, PA 19087, USA.
Jirkovsky
I
I
Tran
B D
BD
Harris
H A
HA
Moran
R A
RA
Komm
B S
BS
D001667:Binding, Competitive; D004958:Estradiol / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology; D020847:Estrogen Receptor Modulators / Q000138:chemical synthesis* / Q000494:pharmacology; D011960:Receptors, Estrogen / Q000187:drug effects; D013438:Sulfhydryl Compounds / Q000138:chemical synthesis*; D013629:Tamoxifen / Q000031:analogs & derivatives
D020847:Estrogen Receptor Modulators; D011960:Receptors, Estrogen; D013438:Sulfhydryl Compounds; D013629:Tamoxifen; D004958:Estradiol