Uncharged nucleoside inhibitors of β-1,4-galactosyltransferase with activity in cellsElectronic supplementary information (ESI) available. See DOI: 10.1039/c5cc09289b

We report 5-substituted uridine derivatives as novel, uncharged inhibitors of β-1,4-galactosyltransferase and chemical tools for cellular applications. The new inhibitors reduce P-selectin glycoprotein 1 (PSGL-1) expression in human monocytes. Our results also provide novel insights into a unique mode of glycosyltransferase inhibition. 5-Substituted uridine derivatives are uncharged galactosyltransferase inhibitors that reduce PSGL-1 expression in human monocytes.