Synthesis and biological activity of conformationally constrained sialyl Lewis X analogues with reduced carbohydrate character.

被引:40
作者
Bamford, MJ [1 ]
Bird, M [1 ]
Gore, PM [1 ]
Holmes, DS [1 ]
Priest, R [1 ]
Prodger, JC [1 ]
Saez, V [1 ]
机构
[1] GLAXO RES & DEV LTD,GLAXO WELLCOME MED RES CTR,DEPT MOLEC SCI,STEVENAGE SG1 2NY,HERTS,ENGLAND
关键词
D O I
10.1016/0960-894X(96)00008-X
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Two conformationally constrained analogues of sialyl Lewis X have been synthesised in which the GlcNAc residue has been replaced with cyclohexyl and phenyl rings. The cyclohexyl derived compound was equipotent to sLex and sLea in vitro, suggesting the main role of the GlcNAc residue in sLex is conformational, and represents a simplified inhibitor of adhesion.
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收藏
页码:239 / 244
页数:6
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