Inhibitory effects of fluorine-substituted estrogens on the activity of 17beta-hydroxy steroid dehydrogenases
Inhibitory effects of fluorine-substituted estrogens on the activity of 17beta-hydroxy steroid dehydrogenases
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DOI：
10.1016/j.mce.2005.11.037
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发表时间：
2006-03-27
影响因子：
4.1
通讯作者：
Adamski, J
中科院分区：
文献类型：
--
作者：
Deluca, D;Möller, G;Adamski, J
在寻找人17 β-羟基类固醇脱氢酶1型（h17 β-HSD 1）的新抑制剂的过程中，研究了一组具有有趣性质的特定类固醇，包括新化合物。合成了在甾体支架的17位具有氟取代的几种雌三烯衍生物，并在体外针对重组h17 β-HSD 1、2、4、5和7进行了测试。鉴定了h17 β-HSD 1和h17 β-HSD 2的中度、大部分非选择性抑制剂和h17 β-HSD 5的选择性抑制剂。讨论了这些化合物对5种h17 β-HSDs的抑制强度和选择性的构效关系。(c)2005爱思唯尔爱尔兰有限公司保留所有权利。
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.