Estrogenic Properties of 3,9-Dihydroxy-7,12-dimethylbenz[a]anthracene in rats2

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Abstract
Previously, the 3,9-dihydroxy derivative of benz[a]anthracene was shown to be weakly estrogenic. The availability of the related diol of the mammary carcinogen dimethylbenz[a]anthracene, i.e., 3,9-dihydroxy-7,12-dimethylbenz[a]anthracene (3,9-diOHDMBA), prompted a similar study of its estrogenic properties. The competitive binding studies of 3,9-diOHDMBA with 17β-estradiol in the uterine cytosol of immature SD rats gave a Ka of 1.7×108m−1, 17β-Estradiol (10−9m) binding to the 8S binding protein was inhibited by 3,9-diOHDMBA at concentrations similar to those of nafoxidine HCI (1×10−5m). Bioassay demonstrated that the diol possesses 1/4,464 the activity of 17β-estradiol.