Estradiol dimers as a new class of steroid sulfatase reversible inhibitors

被引：14
|
作者：
Fournier, Diane
Poirier, Donald [1 ]
机构：
[1] CHUQ CHUL Res Ctr, Div Med Chem, Oncol & Mol Endocrinol Lab, Quebec City, PQ G1V 4G2, Canada
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 03期
基金：
加拿大健康研究院;
关键词：
Sulfatase; Steroid; Inhibitor; Dimer; Enzyme; Cancer; ESTRONE SULFATASE; BREAST-CANCER; MODULATORS; ENZYMES; TISSUE;
D O I：
10.1016/j.bmcl.2008.12.047
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of estradiol dimers was synthesized or selected from compounds available in our laboratory and tested for inhibition against steroid sulfatase. Dimers linked by their C17 position, compounds 7 and 8, showed inhibitory potency similar (56% and 54% at 1 mu M) to that of our best previously reported reversible inhibitor EM-690 (62% at 1 mu M). Docking experiment seems to indicate that C17-C17 dimers bind in a similar way to EM-690 whereas C16-O3 and C16-C16 dimers bind in an upside-down position. (c) 2008 Elsevier Ltd. All rights reserved.
引用
收藏
页码：693 / 696
页数：4
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