Synthesis and Evaluation of Transition-State Analogue Inhibitors of α-1,3-Fucosyltransferase This work was supported by the NIH and the Skaggs Institute. M.L.M. acknowledges fellowships from UNCF⋅Merck Science Initiative and Skaggs Predoctoral Fellows Program.

Mimics of the geometry or charge of the fucose moiety of GDP-fucose in the transition state of fucosyltransferase-catalyzed reactions, compounds 1–3 are good competive inhibitors of α-1,3-fucosyltransferases V and VI with Ki values between 6 and 13 μM. GDP=guanosine diphosphate.