PMID: 2946698Jan 1, 1986Paper

Nonsteroidal antiestrogens and partial estrogens with prostatic tumor inhibiting activity

Journal of Cancer Research and Clinical Oncology
M R SchneiderW Amselgruber

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.

References

Jan 1, 1986·Journal of Cancer Research and Clinical Oncology·M R Schneider
Dec 1, 1984·Journal of Steroid Biochemistry·J D AlbertL E Faber
Jan 1, 1980·British Journal of Pharmacology·J B Dekanski
Dec 1, 1981·Journal of Steroid Biochemistry·A E WakelingL R Hughes
Dec 1, 1981·Journal of Steroid Biochemistry·M M BoutonJ A Grandadam

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Citations

Jan 1, 1990·Journal of Cancer Research and Clinical Oncology·M R SchneiderA H Graf
May 24, 2001·Proceedings of the National Academy of Sciences of the United States of America·Z WeihuaJ A Gustafsson
Oct 10, 2009·Clinical Genitourinary Cancer·Rahul AggarwalCharles J Ryan
Mar 10, 2007·Bioorganic & Medicinal Chemistry Letters·Isamu ShiinaYoshimune Hasome
Jan 4, 2007·International Journal of Urology : Official Journal of the Japanese Urological Association·Domenico PreziosoKeith Griffiths
Oct 1, 1991·Archiv der Pharmazie·C D SchillerM R Schneider
Jun 10, 2014·Nihon Hinyōkika Gakkai zasshi. The japanese journal of urology·Takuji HayashiToshiaki Yoshioka

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