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Design of Mechanism-based Inactivators of Human Placental Aromatase¹

Department of Pharmacology and Experimental Therapeutics, The Johns Hopkins University School Medicine, Baltimore, Maryland 21205

This article reviews the design and study, in our own laboratory and in other laboratories, of new 10ß-substituted analogs of estr-4-ene-3,17-dione. These compounds, along with a number of known analogs, have been evaluated as reversible or irreversible inhibitors of human placental microsomal aromatase. The only irreversible inhibitors in the group surveyed here are the 10ß-difluoromethyl, 10ß-propargyl, and 10ß-allenyl derivatives of estr-4-ene-3,17-dione. Possible mechanisms for the inactivation processes are discussed. The effects of incorporating the 19-methyl group of adrost-4-ene-3,17-dione into a ring of three, four, five or six carbons are also described.