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...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2000-01, Vol.10 (2), p.147-151
Main Authors: MILLER, C. P, JIRKOVSKY, I, TRAN, B. D, HARRIS, H. A, MORAN, R. A, KOMM, B. S
Format: Article
Language:English
Subjects:
Binding, Competitive
Biological and medical sciences
Estradiol - analogs & derivatives
Estradiol - metabolism
Estradiol - pharmacology
Estrogen Receptor Modulators - chemical synthesis
Estrogen Receptor Modulators - pharmacology
Hormones. Endocrine system
Medical sciences
Pharmacology. Drug treatments
Receptors, Estrogen - drug effects
Sulfhydryl Compounds - chemical synthesis
Tamoxifen - analogs & derivatives
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Summary: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.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(99)00648-4