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ID: ALA1146629

Journal: Bioorg Med Chem Lett

Title: Synthesis and evaluation of phosphoramidate amino acid-based inhibitors of sialyltransferases.

Authors: Whalen LJ, McEvoy KA, Halcomb RL.

Abstract: Several phosphoramidate analogues of CMP-N-acetylneuraminic acid were prepared for evaluation as inhibitors of alpha-2,3- and alpha-2,6-sialyltransferase. Central to the synthesis was the oxidative coupling of an amino acid ester with an H-phosphonate to construct the phosphoramidate linkage. All compounds synthesized were weak inhibitors of both of the sialyltransferases as determined by an HPLC-based inhibition assay.

CiteXplore: 12482445

DOI: 10.1016/s0960-894x(02)00735-7