Hormonal characteristics of new modified estrogen 11α -hydroxyderivatives
https://doi.org/10.14341/probl11619
Abstract
Antiestrogen activity in new 11α-hydroxy derivative estrogens was evaluated. Estron and ethynylestradiol 11α-formoxy- and acetoderivatives and 11α-nitroxy- 17β-acetate ethynylestradiol showed pronounced antiestrogen activity; for example, the antiactivity of the latter agent was 40- 55%, depending on its dose. These estrogens 11α-hydroxyderivatives and estradiol 11α-formiate showed no antiestrogen activity. Insertion of the cytotoxic group into the 3rd position of estron and ethynylestradiol 11α- formoxy- and acetoderivatives potentiated their antiestrogen activity. Study of these compounds on transplanted and induced tumors in mice and rats showed their higher antitumorous effects in comparison with tamoxiphene. Estron, estradiol, and ethynylestradiol 11α-formoxy- and 11α-acetoderivatives without cytotoxic group were inactive estrogens.
Supporting agencies: Hormonal characteristics; 11α; estrogens
About the Authors
T. I. IvanenkoEndocrinology Research Center of RAMS
Russian Federation
G. N. Pluzhnikova
Endocrinology Research Center of RAMS
Russian Federation
V. P. Fedotov
Endocrinology Research Center of RAMS
Russian Federation
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Review
For citations:
Ivanenko T.I., Pluzhnikova G.N., Fedotov V.P. Hormonal characteristics of new modified estrogen 11α -hydroxyderivatives. Problems of Endocrinology. 2002;48(3):42-43. (In Russ.) https://doi.org/10.14341/probl11619
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