A CLINICAL EVALUATION OF DIENESTROL, A SYNTHETIC ESTROGEN¹

Abstract

ALTHOUGH the synthetic estrogen, dienestrol, was prepared and described by Dodds and his associates (6) in 1938, it was not until 1942 that Barnes (2) carried out a clinical trial of the estrogen for the inhibition of lactation, reporting in 1944 (3) concerning its effectiveness in the treatment of the menopausal syndrome. The high oral potency of the compound, the absence of untoward or toxic effects, and improved procedures for its preparation have stimulated further clinical investigations of dienestrol. Dodds, et al. (4, 5), in their description of the preparation of this compound, state that they had occasion to prepare pinacols of p-hydroxyacybenzenes, which on dehydration by means of acetyl chloride and acetic anhydride gave substituted 4:4′-dehydroxydiphenylbutadienes which proved to be powerful estrogenic substances. As in the case of the stilbene derivatives, the maximum activity was found when the central chain comprised six carbon atoms giving a compound 4:4′dihydroxy-γ-δ-diphenyl-β:δ-hexadien...