A facile synthesis of C2-Symmetric 17β-Estradiol dimers

被引：19
|
作者：
Rabouin, D
Perron, V
N'Zemba, B
C-Gaudreault, R
Bérubé, G
机构：
[1] Univ Quebec Trois Rivieres, Dept Chim Biol, Trois Rivieres, PQ G9A 5H7, Canada
[2] CHUQ, Hop St Francois Assise, Unite Biotechnol, Inst Biomat Quebec, Quebec City, PQ G1L 3L5, Canada
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 03期
关键词：
D O I：
10.1016/S0960-894X(02)00987-3
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A rapid and efficient synthesis of a series Of C-2-symmetric 17beta-estradiol dimers is described. The new molecules are linked at position 17alpha of the steroid nucleus with either an alkyl chain or a polyethylene glycol chain. They are made from estrone in five chemical steps with an overall yield exceeding 30%. The biological activity of these compounds was evaluated in vitro on estrogen dependent and independent (ER+ and ER-) human breast tumor cell lines: MCF-7 and MDA-MB-231. Some of the dimers present selective cytotoxic activity against the ER+ cell line. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：557 / 560
页数：4
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