New Potent Sialyltransferase Inhibitors—Synthesis of Donor and of Transition-State Analogues of Sialyl Donor CMP-Neu5Ac

Abstract

New concepts for substrate- and transition-state-derived sialyltransferase inhibitors are deduced from enzymatic sialyl transfer with CMP-Neu5Ac as donor substrate. On this basis, transition-state analogue (R)-1 was synthesized, which inhibits α(2–6)-sialyltransferase from rat liver, an important lead for further investigations.