PMID: 3754557Jan 1, 1986Paper

Studies on the mammary tumor-inhibiting effects of diethylstilbestrol and its mono- and diphosphate

Journal of Cancer Research and Clinical Oncology
M R SchneiderW P Brade

Abstract

Diethylstilbestrol (DES), diethylstilbestrol monophosphate (DES-MP) and diethylstilbestrol diphosphate (DES-DP) were tested for their estrogen receptor affinity, estrogenic potency and mammary tumor-inhibiting activity in vitro and in vivo. DES had a much higher receptor binding affinity than its mono- or diphosphate. All three compounds inhibited the growth of the hormone-dependent MCF-7 and hormone-independent MDA-MB 231 breast cancer line only at relatively high concentrations. The estrogenic potency in the immature mouse uterine weight test decreased in the order DES greater than DES-MP much greater than DES-DP. The hormone-dependent MXT mammary tumor of the mouse was inhibited by all three compounds at a dosage of 1.0 mg/kg per week. At a dose of 0.01 mg/kg, DES, DES-MP, and DES-DP stimulated the tumor growth. Thus, for the first time, a biphasic effect on tumor growth was demonstrated in intact mature animals. As the effects of all three compounds were similar in this assay, a cleavage of the phosphate groups is likely. A decrease in estrogenic potency concomitant with a retained antitumor effect of DES-MP and DES-DP compared to DES was not demonstrable in the mature mouse using the MXT assay, only in the uterotrophic tes...Continue Reading

References

Jan 1, 1979·Cancer Chemotherapy and Pharmacology·L M van PuttenF Spreafico
Sep 1, 1979·Journal of Cancer Research and Clinical Oncology·S PoppemaK Lennert
Dec 1, 1976·Current Problems in Cancer·G Leclercq, J C Heuson
Dec 1, 1976·Proceedings of the National Academy of Sciences of the United States of America·C K OsborneM E Lippman
Dec 1, 1985·Journal of Medicinal Chemistry·M R SchneiderH Schönenberger
Jul 1, 1970·The Journal of Urology·C PromislowA Clarke
Jan 1, 1981·Journal of Cancer Research and Clinical Oncology·M R SchneiderG Ruckdeschel
Aug 1, 1983·Endocrinology·S M SchollM E Lippman
Dec 5, 1952·Deutsche medizinische Wochenschrift·H DRUCKREY

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