Synthesis of 2,2-dimethyl-4-hydroxy-4-androstene-3,17-dione as an inhibitor of aromatase.

Autor: Furth PS; Dept of Pharmacology and Molecular Sciences, Johns Hopkins University School of Medicine, Baltimore, MD 21205., Rosenberger J, Marcotte PA, Robinson CH
Jazyk: angličtina
Zdroj: Journal of enzyme inhibition [J Enzyme Inhib] 1990; Vol. 4 (2), pp. 131-5.
DOI: 10.3109/14756369009040734
Abstrakt: 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.
Databáze: MEDLINE