The biologic activity of selenoestrogens

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Abstract
For differential imaging of mammary tumors with estrogen receptors and without estrogen receptors .gamma.-emitting estrogen analogs were required. The binding properties of 7.alpha.-, 16.alpha.-, and 17.alpha.-methylselenoestrogens and 17.alpha.-phenylselenoestrogens relative to the binding properties of estradiol are reported. The selenium-containing estrogens retained the ability to displace [3H] estradiol from the estrogen receptor of rabbit uterine cytosol, although in most instances the displacement was small (3-7% compared to estradiol). The most active compounds were 16.alpha.-phenylselenoestrone, 16.alpha.-methylselenoestradiol, and 17.alpha.-methylselenomethylestradiol which had relative binding of 23, 27 and 31%, respectively, compared with that of estradiol. 16.alpha.-Methylselenoestradiol was able to translocate the estrogen cytosol receptor to the nucleus, in vitro, but was not able to increase the uterine weight when administered to mice in vitro.