Collect. Czech. Chem. Commun. 2006, 71, 532-542

The Influence of 17-Oxo- and 17-Hydroxy-16,17-secoestratriene Derivatives on Estrogen Receptor

Suzana Jovanović-Šantaa,*, Julijana Petrovića, Marija Sakača, Zorica Žakulab, Esma Isenovićb and Nevena Ribarac-Stepićb

a Department of Chemistry, Faculty of Science, University of Novi Sad, Trg Dositeja Obradovića 3, 21000 Novi Sad, Serbia and Montenegro
b Laboratory for Molecular Biology and Endocrinology, Institute for Nuclear Sciences "Vinča", P.O. Box 522, 11000 Belgrade, Serbia and Montenegro


Since many of newly synthesised D-secoestratriene derivatives showed antiestrogenic effect, with almost a total loss of estrogenic activity, we studied the effects of some of these compounds on estrogen receptors (ER), the translocation of the estrogen-ER complexes formed in presence of competing substances into the nucleus, as well as the binding of these complexes to DNA. The results of uterotrophic effects of analysed derivatives are in agreement with the influence of these compounds on activity and binding parameters of estrogen receptors. Namely, compounds that show relatively high antiestrogenic activity predominantly increase Kd and inhibit translocation to nuclei of radioactive complexes formed in their presence. On the other hand, compounds that do not significantly change binding parameters of estrogen receptors do not show antiestrogenic effect in in vivo experiments.

Keywords: Steroids; Estrogens; Antiestrogens; D-secoestratriene derivatives; Estrogen receptor binding; Steroid-receptor interaction; Receptor activation; Nuclear translocation.

References: 31 live references.