title: Nonsteroidal antiestrogens and partial estrogens with prostatic tumor inhibiting activity.
abstract: Antiestrogens and partial estrogens of the stilbene (1 and 4), triphenylbutene (2) and diphenylethane (3) series were tested for their potential prostatic tumor inhibiting activity. Compounds 1 and 2 exerted a strong inhibitory activity on prostate and seminal vesicle weight of intact rats and mice, whereas the strong antiestrogen 3 and compound 4 had no or only a slight effect. The tumor inhibiting activity of 1 and 2 on the hormone-dependent R 3327 Dunning prostatic carcinoma of the rat was strong and comparable to that of castration or administration of the potent estrogen DES. Compounds 1-4 had no direct antiandrogenic effect in castrated, testosterone-substituted rats and mice, and no affinity for the androgen or progesterone receptor. To the estrogen receptor from prostatic tumor cytosol, however, 1-4 had good receptor affinities. As the partial antiestrogen 1 and the partial estrogen 2 have much lower estrogenic properties than DES, but still have strong prostatic tumor inhibiting properties, they may offer a suitable alternative to conventional therapy of prostate carcinoma because of their possibly low estrogenic side effects.
mesh_terms: D000818:Animals; D003534:Cyproterone / Q000031:analogs & derivatives / Q000627:therapeutic use; D017373:Cyproterone Acetate; D004054:Diethylstilbestrol / Q000627:therapeutic use; D004958:Estradiol / Q000032:analysis; D004965:Estrogen Antagonists / Q000627:therapeutic use*; D004967:Estrogens / Q000627:therapeutic use*; D005837:Genitalia, Male / Q000187:drug effects / Q000473:pathology; D008297:Male; D051379:Mice; D009929:Organ Size / Q000187:drug effects; D011374:Progesterone / Q000032:analysis; D011471:Prostatic Neoplasms / Q000139:chemically induced / Q000188:drug therapy*; D051381:Rats; D013267:Stilbenes / Q000627:therapeutic use; D013629:Tamoxifen / Q000627:therapeutic use; D013739:Testosterone / Q000627:therapeutic use
chemical_list: D004965:Estrogen Antagonists; D004967:Estrogens; D013267:Stilbenes; D013629:Tamoxifen; D013739:Testosterone; D011374:Progesterone; D017373:Cyproterone Acetate; D004958:Estradiol; D004054:Diethylstilbestrol; D003534:Cyproterone