Document Report Card

ID: ALA1129038

Journal: J Med Chem

Title: Studies on selectin blocker. 1. Structure-activity relationships of sialyl Lewis X analogs.

Authors: Ohmoto H, Nakamura K, Inoue T, Kondo N, Inoue Y, Yoshino K, Kondo H, Ishida H, Kiso M, Hasegawa A.

Abstract: As part of our studies of selectin blockers, we prepared 1-deoxy-3'-O-sulfo LeX analogs (1-3), 1-deoxy-3'-O-phosphono LeX analogs (4), and 1-deoxy sLeX analogs (5-7), and examined their inhibitory activities against natural ligand (sLeX) binding to E-selectin, P-selectin, and L-selectin. The 1-deoxy sLeX 5 was up to 20 times more potent an inhibitor than the sLeX tetrasaccharide toward P- and L-selectin binding. This indicates that the modification of the 1 or 2 position of sLeX is useful in the design of a more potent selectin blocker.

CiteXplore: 8632441

DOI: 10.1021/jm9506478