期刊
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
卷 31, 期 6, 页码 1170-1176出版社
TAYLOR & FRANCIS LTD
DOI: 10.3109/14756366.2015.1103235
关键词
5 alpha-Reductase inhibitors; 5 alpha-reductase type 2; 16-formyl-17-methoxy dehydroepiandrosterone ester derivatives; androgen receptor; prostate cancer
资金
- Consejo Nacional de Ciencia y Tecnologia (CONACYT) [165049]
- Direccion General de Asuntos del Personal Academico (DGAPA project) [IN 211312]
In this study, we investigated the in vitro effect of 16-formyl-17-methoxy dehydroepiandrosterone derivatives on the activity of 5 alpha-reductase type 2 (5 alpha-R2) obtained from human prostate. The activity of different concentrations of these derivatives was determined for the conversion of labelled testosterone to dihydrotestosterone. The results indicated that an aliphatic ester moiety at the C-3 position of these derivatives increases their in vitro potency as inhibitors of 5 alpha-R2 activity compared to finasteride (R), which is considered to be a potent inhibitor of 5 alpha-R2. In this case, the augmentation of the lipophilicity of these dehydroepiandrosterone derivatives increased their potency as inhibitors of 5 alpha-R2. However, the presence of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl rings as the cycloaliphatic ester moiety at C-3 of the formyl methoxy dehydroepiandrosterone scaffold did not inhibit the activity of this enzyme. This may be due to the presence of steric factors between the enzyme and the spatial structure of these derivatives.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据