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

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.
AuthorsTamara Delaine, Ian Cumpstey, Laurent Ingrassia, Marie Le Mercier, Paul Okechukwu, Hakon Leffler, Robert Kiss, Ulf J Nilsson
JournalJournal of medicinal chemistry (J Med Chem) Vol. 51 Issue 24 Pg. 8109-14 (Dec 25 2008) ISSN: 1520-4804 [Electronic] United States
PMID19053747 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Esters
  • Galectins
  • Thiogalactosides
  • thiodigalactoside
Topics
  • Cell Line, Tumor
  • Cell Movement
  • Drug Design
  • Drug Screening Assays, Antitumor
  • Esters
  • Galectins (chemistry)
  • Humans
  • Inhibitory Concentration 50
  • Kinetics
  • Lung Neoplasms (therapy)
  • Male
  • Models, Chemical
  • Prostatic Neoplasms (therapy)
  • Protein Structure, Tertiary
  • Thiogalactosides (chemistry, metabolism)

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