Ethacrynic acid analogues lacking the α,β-unsaturated carbonyl unit-Potential anti-metastatic drugs

被引:12
作者
Janser, Romy F. J. [1 ]
Meka, Ranjith K. [1 ]
Bryant, Zack E. [1 ]
Adogla, Enoch A. [1 ]
Vogel, Elizabeth K. [1 ]
Wharton, Jaimie L. [1 ]
Tilley, Cynthia M. [1 ]
Kaminski, Catherine N. [2 ]
Ferrey, Seth L. [2 ]
Van Slambrouck, Severine [2 ]
Steelant, Wim F. A. [2 ]
Janser, Ingo [1 ]
机构
[1] New Mexico Inst Min & Technol, Dept Chem, Lab Organ Synth Catalysis & Biochem, Socorro, NM 87801 USA
[2] New Mexico Inst Min & Technol, Dept Chem, Lab Biochem & Biomed Res, Socorro, NM 87801 USA
基金
美国国家科学基金会; 美国国家卫生研究院;
关键词
Ethacrynic acid; Metastases; Inhibition; Anti-cancer; Drug; GLUTATHIONE-S-TRANSFERASE; P1-1; ACTIVITY; CELLS;
D O I
10.1016/j.bmcl.2010.01.144
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of ethacrynic acid analogues, lacking the alpha,beta-unsaturated carbonyl unit, was synthesized and subsequently evaluated for their ability to inhibit the migration of human breast cancer cells, MCF-7/AZ. Several of the analogues were already active in the low micromolar range, whereas ethacrynic acid itself shows no potential to inhibit the migration of these cancer cells. Preliminary studies show that the presence of one or more methoxy groups at the phenyl ring of ethacrynic acid is important in order for the ethacrynic acid analogues to demonstrate an inhibitory effect on the migration. (C) 2010 Elsevier Ltd. All rights reserved.
引用
收藏
页码:1848 / 1850
页数:3
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