2,2-二甲基-4-羟基-4-雄烯-3,17-二酮作为芳香化酶抑制剂的合成。

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

作者信息

Furth P S, Rosenberger J, Marcotte P A, Robinson C H

机构信息

Dept of Pharmacology and Molecular Sciences, Johns Hopkins University School of Medicine, Baltimore, MD 21205.

出版信息

J Enzyme Inhib. 1990;4(2):131-5. doi: 10.3109/14756369009040734.

DOI:10.3109/14756369009040734

PMID:2098519

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.

摘要

2,2 - 二甲基 - 4 - 羟基 - 4 - 雄烯 - 3,17 - 二酮（4）已被合成，并且已被证明是芳香化酶的一种强效竞争性抑制剂（抑制常数Ki = 11.4纳摩尔）。然而，与未甲基化的母体化合物4 - 羟基雄烯二酮（4 - OHA）相反，化合物4不会导致酶活性随时间的丧失。