Nonsteroidal estrogens and antiestrogens: biological activity of cyclopropyl analogs of stilbene and stilbenediol.
The estrogenic, antiestrogenic, and receptor binding activity of a series of cyclopropyl analogs of stilbene and stilbenediol were determined using the uterotropic assay in the mouse and the receptor binding assay with rat uterine cytosol. One compound, 1,1-dichloro-cis-2,3-diphenylcyclopropane (II), displayed antiestrogenic activity in vivo with a low affinity for the estrogen receptor in vitro and showed tumor remission activity on 7,12-dimethylbenz(a)anthracene-induced estrogen-dependent rat mammary tumors. Compounds VIII, IV, and V (in that order) exhibited the greatest estrogen activity in the mouse and the greatest receptor binding activity in vitro. Compound VIII exhibited antifertility activity in the mouse.
D000818:Animals; D000970:Antineoplastic Agents; D002369:Castration; D004965:Estrogen Antagonists; D004968:Estrogens, Non-Steroidal; D005260:Female; D005298:Fertility / Q000187:drug effects; D051379:Mice; D051381:Rats; D011960:Receptors, Estrogen / Q000187:drug effects; D013267:Stilbenes / Q000494:pharmacology*; D014590:Uterine Contraction / Q000187:drug effects; D014599:Uterus / Q000033:anatomy & histology
D000970:Antineoplastic Agents; D004965:Estrogen Antagonists; D004968:Estrogens, Non-Steroidal; D011960:Receptors, Estrogen; D013267:Stilbenes