Synthesis of 17β-estradiol platinum(II) complexes:: Biological evaluation on breast cancer cell

被引：69

作者：

Descôteaux, C

Provencher-Mandeville, J

Mathieu, I

Perron, V

Mandal, SK

Asselin, É

Bérubé, G

机构：

[1] Univ Quebec Trois Rivieres, Dept Chim Biol, Trois Rivieres, PQ G9A 5H7, Canada

[2] Coll N Atlantic, Div Sci & Technol, Clarenville, NF A5A 1V9, Canada

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 22期

基金：

加拿大自然科学与工程研究理事会;

关键词：

D O I：

10.1016/j.bmcl.2003.09.011

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

The synthesis of a novel series of 17beta-estradiol-linked platinum(II) complexes is described. The new molecules are linked with an alkyl chain at position 16alpha of the steroid nucleus and bear a 16beta-hydroxymethyl side chain. They are made from estrone in five chemical steps with an overall yield exceeding 28%. The biological activity of these compounds was evaluated in vitro on estrogen dependent and independent (ER+ and ER-) human breast cancers. The derivatives incorporating a 2-(2'-aminoethyl)pyridine ligand displayed good activity against the cell lines particularly when the connecting arm is 10 carbon atoms long. (C) 2003 Elsevier Ltd. All rights reserved.

引用

页码：3927 / 3931

页数：5

共 19 条

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