Inhibitory effects of ethacrynic acid analogues lacking the α,β-unsaturated carbonyl unit and para-acylated phenols on human cancer cells

被引:10
作者
Bryant, Zack E. [1 ]
Janser, Romy F. J. [1 ]
Jabarkhail, Medina [1 ]
Candelaria-Lyons, Melissa S. [2 ]
Romero, Brittni B. [2 ]
Van Slambrouck, Severine [2 ]
Steelant, Wim F. A. [2 ,3 ]
Janser, Ingo [1 ]
机构
[1] New Mexico Inst Min & Technol, Lab Organ Synth Catalysis & Biochem LOSCB, Dept Chem, Socorro, NM 87801 USA
[2] New Mexico Inst Min & Technol, Lab Biochem & Biomed Res, Dept Chem, Socorro, NM 87801 USA
[3] St Thomas Univ, Sch Sci Technol & Engn Management, Miami Gardens, FL 33054 USA
基金
美国国家卫生研究院;
关键词
GLUTATHIONE-S-TRANSFERASE; PROSTATE-CANCER; P1-1; ACTIVITY; INVASION; PROLIFERATION; CYSTEINE; BREAST;
D O I
10.1016/j.bmcl.2010.12.074
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, Hs578Ts(i) 8 as well as of human prostate cancer cells, C4-2B. These cell lines provide a good model system to study migration and invasion, since they represent metastatic cancer. Our studies show that ethacrynic acid analogues with methyl substituents at the aromatic ring demonstrate no inhibitory effect on the migration of both cancer cell lines, whereas a precursor in the synthesis of these ethacrynic acid analogues (II-1, a para-acylated m-cresol) is an excellent inhibitor of the migration of both cancer cell lines. (C) 2010 Elsevier Ltd. All rights reserved.
引用
收藏
页码:912 / 915
页数:4
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