[Development of new antiestrogens of the 3,3'-dihydroxy-alpha, beta-diethylstilbene-type and their evaluation on the DMBA-induced hormone dependent mammary carcinoma of the SD-rat (author's transl)].
The displacement of the phenolic OH-group of diethylstilbestrol into the 3,3'-position (trans-3,3'-dihydroxy-alpha, beta-diethylstilbene, compd. III) leads to a strong decrease of the estrogenic effect under conservation of the receptor affinity. In vitro, III inhibits the estradiol-receptor-interaction competitively and, in vivo, antagonises the uterotropic effect of estrone in the mouse. In tests with the DMBA-induces, hormone-dependent mammary carcinoma of the rat a dose-dependent strong decrease of tumor size and yield is achieved under the influence of III, due to the antiestrogenic properties of III. The replacement of the alpha, beta-bound ethyl groups in III by other alkyl chains leads to no further increase of the antiestrogenic and antitumor activity.
D000230:Adenocarcinoma / Q000139:chemically induced*; D000818:Animals; D001943:Breast Neoplasms / Q000139:chemically induced*; D004054:Diethylstilbestrol / Q000494:pharmacology* / Q000031:analogs & derivatives; D004965:Estrogen Antagonists / Q000494:pharmacology*; D051379:Mice; D009374:Neoplasms, Experimental; D051381:Rats
D004965:Estrogen Antagonists; D004054:Diethylstilbestrol; C028517:3,3'-dihydroxy-alpha,beta-diethylstilbene
Entwicklung neuer Antiöstrogene vom Typ des 3,3'-Dihydroxy-alpha, beta-diäthylstilbens und ihre Prüfung am DMBA-induzierten, hormonabhängigen Mammacarcinom der SD-Ratte.