Synthesis of 2,2-Dimethyl-4-Hydroxy-4-Androstene-3,17-Dione as An Inhibitor of Aromatase

Paul S. Furth Dept of Pharmacology and Molecular Sciences, The Johns Hopkins University School of Medicine, Baltimore, MD, 21205, USA

John Rosenberger Dept of Pharmacology and Molecular Sciences, The Johns Hopkins University School of Medicine, Baltimore, MD, 21205, USA

Patrick A. Marcotte Dept of Pharmacology and Molecular Sciences, The Johns Hopkins University School of Medicine, Baltimore, MD, 21205, USA

Cecil H. Robinson Dept of Pharmacology and Molecular Sciences, The Johns Hopkins University School of Medicine, Baltimore, MD, 21205, USA

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 (K_i = 11.4nM). However, compound 4 does not cause time-dependent loss of enzyme activity, in contrast to the unmethylated parent compound, 4-OHA.

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Synthesis of 2,2-Dimethyl-4-Hydroxy-4-Androstene-3,17-Dione as An Inhibitor of Aromatase

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Synthesis of 2,2-Dimethyl-4-Hydroxy-4-Androstene-3,17-Dione as An Inhibitor of Aromatase

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