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ID: ALA4020702
Journal: Bioorg Med Chem
Title: Development of α1,6-fucosyltransferase inhibitors through the diversity-oriented syntheses of GDP-fucose mimics using the coupling between alkyne and sulfonyl azide.
Authors: Manabe Y, Kasahara S, Takakura Y, Yang X, Takamatsu S, Kamada Y, Miyoshi E, Yoshidome D, Fukase K.
Abstract: We developed α1,6-fucosyltransferase (FUT8) inhibitors through a diversity-oriented synthesis. The coupling reaction between the fucose unit containing alkyne and the guanine unit containing sulfonyl azide under various conditions afforded a series of Guanosine 5'-diphospho-β-l-fucose (GDP-fucose) analogs. The synthesized compounds displayed FUT8 inhibition activity. A docking study revealed that the binding mode of the inhibitor synthesized with FUT8 was similar to that of GDP-fucose.
CiteXplore: 28284868