Inhibitory effects of fluorine-substituted estrogens on the activity of 17beta-hydroxy steroid dehydrogenases

被引：31

作者：

Deluca, D

Möller, G

Rosinus, A

Elger, W

Hillisch, A

Adamski, J

机构：

[1] GSF, Natl Res Ctr Environm & Hlth, Inst Expt Genet, Genome Anal Ctr, D-85764 Neuherberg, Germany

[2] EnTec GmbH, D-07745 Jena, Germany

来源：

MOLECULAR AND CELLULAR ENDOCRINOLOGY | 2006年 / 248卷 / 1-2期

关键词：

17beta-hydroxysteroid dehydrogenase; inhibitor; fluorine-substitution;

D O I：

10.1016/j.mce.2005.11.037

中图分类号：

Q2 [细胞生物学];

学科分类号：

071009 ; 090102 ;

摘要：

In search for new inhibitors of human 17beta-hydroxysteroid dehydrogenase type 1 (h17 beta-HSD1) a specific group of steroids with interesting properties including novel compounds was investigated. Several estratriene derivatives with fluorine-substitution in position 17 of the steroidal scaffold were synthesised and tested in vitro towards recombinant h17 beta-HSD1, 2,4,5 and 7. Moderate, mostly unselective inhibitors of h17 beta-HSD1 and h I 7 beta-HSD2 and a selective inhioitor of h17 beta-HSD5 were identified. The structure-activity relationship with respect to inhibitory strengths and selectivity of these compounds on five h17 beta-HSDs is discussed. (c) 2005 Elsevier Ireland Ltd. All rights reserved.

引用

页码：218 / 224

页数：7

共 29 条

[1]

ADAMS J, 1981, CANCER RES, V41, P4720

[2] Physiology and molecular genetics of 17 beta-hydroxysteroid dehydrogenases [J].