Synthesis of O-galactosyl aldoximes as potent LacNAc-mimetic galectin-3 inhibitors.
نویسندگان
چکیده
A panel of anomeric oxime ether derivatives of beta-galactose were synthesized via the reaction of O-beta-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-(beta-D-galactopyranosyl)-indole-3-carbaldoxime (E-52), had a Kd value of 180 microM, which is 24 times better than methyl beta-D-galactopyranoside (Kd=4400 microM) and in the same range as methyl lactoside (Kd=220 microM).
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ورودعنوان ژورنال:
- Bioorganic & medicinal chemistry letters
دوره 15 9 شماره
صفحات -
تاریخ انتشار 2005