Abstract
A panel of anomeric oxime ether derivatives of β-galactose were synthesized via the reaction of O-β- d-galactopyranosylhydroxylamine with aldehydes. The oxime ethers were evaluated as inhibitors against galectin-3 in a competitive fluorescence polarization assay. The best inhibitor, [ E]- O-(β- d-galactopyranosyl)-indole-3-carbaldoxime ( E- 52), had a K d value of 180 μM, which is 24 times better than methyl β- d-galactopyranoside ( K d = 4400 μM) and in the same range as methyl lactoside ( K d = 220 μM).
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