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American Chemical Society, Journal of Medicinal Chemistry, 24(51), p. 8109-8114, 2008

DOI: 10.1021/jm801077j

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

Journal article published in 2008 by Tamara Delaine, Ian Cumpstey, Laurent Ingrassia, Marie Le Mercier, Marie Le Mercier, Paul Okechukwu, Hakon Leffler, Robert Kiss, Ulf J. Nilsson ORCID
This paper was not found in any repository; the policy of its publisher is unknown or unclear.
This paper was not found in any repository; the policy of its publisher is unknown or unclear.

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Abstract

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. ; Journal Article ; Research Support, Non-U.S. Gov't ; info:eu-repo/semantics/published