Bisubstrate-type inhibitor of sialyltransferases

A convergent strategy for the construction of bisubstrate-type sialyltransferase inhibitor (1) was developed. It consists of consecutive coupling of three components (N-acetyllactosamine, sialic acid, and CMP), followed by oxidation and deprotection. As expected, compound 1 showed potent inhibitory activities toward both 2,3-(N)- and 2,6-(N)-sialyltransferase.