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A. R. Abarbanel, Clinical Evaluation of Adjunctive Therapy with Stilbestrol Monomethyl Ether with Comments on Toxicity, The Journal of Clinical Endocrinology & Metabolism, Volume 2, Issue 6, 1 June 1942, Pages 386–391, https://doi.org/10.1210/jcem-2-6-386
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Abstract
That all biological processes are essentially chemical in nature is becoming increasingly evident, especially in the field of reproductive physiolbgy. Among the more significant of these advances has been the demonstration that estrogenic activity is the property of scores of compounds, many of which do not possess a steroid nucleus. The latter group includes the very potent synthetic estrogen, diethyldihydroxystilbene, which is also known as diethylstilhestrol.
The ultimate desideratum of estrogenic therapy is a compound that is efficacious orally, inexpensive and practically free from side reactions. To date, diethylstilbestrol has proven to be the compound most suitably meeting these requirements. In a small percentage of patients certain undesirable side-effects may occur usually of a gastrointestinal nature. In an effort to reduce these side-effects to a minimum the compound stilbestrol monomethyl ether has been prepared and submitted for clinical trial.
Since it has been shown that estrone methyl ether is probably demethylated into free estrone before being metabolized, it seemed plausible that demethylation of stilbestrol monomethyl ether was a prerequisite for its estrogenic action (1, 2).
