Raymond E. Counsell

An Azasterol that Inhibits Cholesterol Synthesis in vitro.

Summary A new inhibitor of cholesterol synthesis, SC-11952, closely related structurally to cholesterol, has been characterized in terms of its effects on acetate and meva-lonate metabolism in vitro. The compound did not reduce acetate conversion to CO2, fatty acids, or keto-acids but did inhibit incorporation of this substrate into cholesterol. Inhibition of mevalonate conversion to cholesterol was less than when acetate was the substrate. The similarity of the effects of SC-11952 to those produced by cholesterol feeding is discussed.

Anti-Androgenic Activity of a Series of 17-Iminosteroids

Summary A series of five 17-iminoste-roids was tested in combination with testosterone propionate in castrated male rats. All of these compounds inhibited the response to testosterone propionate in the seminal vesicles and ventral prostate glands. There was no indication of inhibition of pituitary gonadotropin secretion in spayed female rats treated with several of these compounds. While inhibition of the action of exogenous testosterone propionate was obtained, no effect on endogenous androgen was observed in intact males at the dose used.

The estrogenic and deciduogenic properties of some estra-1,3,5(10)triene-3,17β-diol derivatives

Die östrogene Aktivität von einigen substituierten Östrodiolderivaten wurde in Rattenvaginalabstrichen und Mäuseuterus-Wachstumversuchen nachgewiesen. Die Einführung von 17α-Alkyl-, Alkenyloder Alkinylgruppen in die Östradiolgruppierung hatte einen signifikanten Effekt auf die östrogene Aktivität. Das 17-(2-Butinyl)-Derivat von Östradiol war eine der wirksamsten Substanzen in den Östrogen- und Deciduomaversuchen.