Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 51, Issue 24, Pages 8109-8114Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm801077j
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Funding
- Lund University
- Swedish Research Council
- Swedish Strategic Research Foundation
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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.
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