A novel fluorinated derivative of diethylstilbestrol. |
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| Authors: | J A McLachlan K Baucom K S Korach L Levy M Metzler |
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| Affiliation: | 1. National Institute of Environmental Heatlh Sciences, Research Triangle Park, North Carolina 27709 U.S.A.;2. PCR Corporation, Gainesville, Florida32602 U.S.A.;3. Institute of Toxicology, University of Würzburg, Würzburg, Germany |
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| Abstract: | The synthesis of the diethylstilbestrol (DES) derivative with fluorine atoms present in the positions ortho to the hydroxyl in each ring is described. In vitro studies in a system containing horse radish peroxidase/H2O2 demonstrate extensive oxidation of tetrafluorodiethylstilbestrol to the corresponding dienestrol derivative. Tetrafluorodiethylstilbestrol and DES had comparable in vivo uterotropic activities at a dose of 100 microgram/kg. Competitive binding experiments demonstrated 20-25 fold reduced interaction with the mouse uterine estrogen receptor. This compound may be useful as an experimental estrogen in distinguishing between the biological and toxic effects of DES. |
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| Keywords: | To whom correspondence should be addressed. |
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