title: Synthesis of 2,2-dimethyl-4-hydroxy-4-androstene-3,17-dione as an inhibitor of aromatase.
abstract: 2,2-Dimethyl-4-hydroxy-4-androstene-3,17-dione (4) has been synthesized and has been shown to be a powerful competitive inhibitor of aromatase (Ki = 11.4 nM). However, compound 4 does not cause time-dependent loss of enzyme activity, in contrast to the unmethylated parent compound, 4-OHA.
authors.affiliation: Dept of Pharmacology and Molecular Sciences, Johns Hopkins University School of Medicine, Baltimore, MD 21205.
authors.forename: P S
authors.initials: PS
authors.lastname: Furth
authors.forename: J
authors.initials: J
authors.lastname: Rosenberger
authors.forename: P A
authors.initials: PA
authors.lastname: Marcotte
authors.forename: C H
authors.initials: CH
authors.lastname: Robinson
mesh_terms: D000735:Androstenedione / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D047072:Aromatase Inhibitors; D001667:Binding, Competitive; D005260:Female; D006801:Humans; D007700:Kinetics; D008861:Microsomes / Q000201:enzymology; D015394:Molecular Structure; D010920:Placenta / Q000201:enzymology; D011247:Pregnancy; D013329:Structure-Activity Relationship
chemical_list: D047072:Aromatase Inhibitors; C069518:2,2-dimethyl-4-hydroxy-4-androstene-3,17-dione; D000735:Androstenedione