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Effects of 4-Nitroestrone 3-Methyl Ether on Dimethylbenz(a)anthracene-induced Mammary Tumors¹

Department of Chemistry, Michigan Cancer Foundation [J. R., E. H. L., J. C., D. O., J. P. H., S. C. B.] and Departments of Biochemistry [J. R., S. C. B.] and Oncology [J. P. H.], Wayne State University School of Medicine, Detroit, Michigan 48201, and Hughes Research and Development, Kalamazoo, Michigan 49009 [R. H., D. E. H., E. W.]

4-Nitroestrone 3-methyl ether has been shown to be an effective growth inhibitor of certain dimethylbenz(a)anthracene-induced rat mammary tumors in intact or ovariectomized rats. When administered at optimum levels (24 mg/kg daily), this Aring-substituted estrone displayed no toxicity, slight estrogenicity, and an antitumor activity which was comparable to that of tamoxifen and nafoxidine and was surpassed only by ovariectomy or pharmacological doses of 17ß-estradiol 3-benzoate. In addition, the appearance of mammary tumors was prevented when this estrogen derivative was administered to rats just prior to or after dimethylbenz(a)anthracene intubation. Unique to the action of the methyl ether of 4-nitroestrone on mammary tumors was the destruction of adenocarcinomas while permitting the appearance of fibroadenomas. Systemically, 4-nitroestrone 3-methyl ether brought about focal atrophy within the pituitary and ovaries while causing moderate hypertrophy of the uterus. Plasma prolactin was unaffected.

¹ Supported by NIH Grants USPHS CA 23079 and CA 22828 from the National Cancer Institute and in part by an institutional grant to the Michigan Cancer Foundation from the United Foundation of Greater Detroit. Reported in part at the 16th Annual Meeting of the American Association for Cancer Research, San Diego, Calif., May 1980 (24).

² To whom requests for reprints should be addressed, at Michigan Cancer Foundation, 110 E. Warren Avenue, Detroit, Mich. 48201.

Received 7/31/81. Accepted 2/14/83.