Galectin-inhibitory thiodigalactoside ester derivatives have antimigratory effects in cultured lung and prostate cancer cells.

Summary, in English

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 on human PC-3 prostate and human A549 nonsmall-cell lung cancer cells.

• Author: Tamara Delaine; Ian Cumpstey; Laurent Ingrassia; Marie Le Mercier; Paul Okechukwu; Hakon Leffler; Robert Kiss; Ulf Nilsson
• Department/s: Centre for Analysis and Synthesis; Division of Microbiology, Immunology and Glycobiology - MIG
• Publishing year: 2008
• Language: English
• Pages: 8109-8114
• Publication/Series: Journal of Medicinal Chemistry
• Volume: 51
• Issue: 24
• Links: http://dx.doi.org/10.1021/jm801077j
• Document type: Journal article
• Publisher: The American Chemical Society (ACS)
• Topic: Medicinal Chemistry
• Status: Published
• ISBN/ISSN/Other: ISSN: 1520-4804