Galectin-Inhibitory Thiodigalactoside Ester Derivatives Have Antimigratory Effects in Cultured Lung and Prostate Cancer Cells

被引：59

作者：

Delaine, Tamara ^{[1
]}

Cumpstey, Ian ^{[1
]}

Ingragsia, Laurent ^{[2
]}

Le Mercier, Marie ^{[4
]}

Okcchukwu, Paul ^{[1
]}

Leffler, Hakon ^{[3
]}

Kiss, Robert ^{[4
]}

Nilsson, Ulf J. ^{[1
]}

机构：

[1] Lund Univ, SE-22100 Lund, Sweden

[2] Unibioscreen SA, B-1070 Brussels, Belgium

[3] Lund Univ, Dept Lab Med, Sect MIG, SE-22362 Lund, Sweden

[4] Univ Libre Bruxelles, Inst Pharm, Toxicol Lab, Brussels, Belgium

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2008年 / 51卷 / 24期

基金：

瑞典研究理事会;

关键词：

D O I：

10.1021/jm801077j

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Aromatic 3,3'-diesters of thiodigalactoside were synthesized in a rapid three-step sequence from commercially available thiodigalactoside and evaluated as inhibitors of cancer- and immunity-related galectins. For each of galectins-1, -3, -7, and -9N-terminal domain, aromatic 3,3'-diesters of thiodigalactoside were found to have affinities in the low micromolar range, which represents a 7-70 fold enhancement over thiodigalactoside itself. No significant improvement was found for galectin-8 N-terminal domain. Two of the compounds were selected for testing in cell Culture and were shown to have potent antimigratory effects oil human PC-3 prostate and human A549 nonsmall-cell lung cancer cells.

引用

页码：8109 / 8114

页数：6

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