摘要:
A series of O2 and O3-derivatized methyl beta-D-talopyranosides were synthesized and evaluated in vitro as inhibitors of the galactose-binding galectin-1, -2, -3, -4 ( N- and C-terminal domains), 8 ( N- terminal domain), and 9 ( N- terminal domain). Galectin-4C and 8N were found to prefer the D-talopyranose configuration to the natural ligand D-galactopyranose configuration. Derivatization at talose O2 and/or O3 provided selective submillimolar inhibitors for these two galectins. (C) 2008 Elsevier Ltd. All rights reserved.