Design and synthesis of a new sialyl Lewis X mimetic: How selective are the selectin receptors?

被引：18
|
作者：
De Vleeschauwer, M
Vaillancourt, M
Goudreau, N
Guindon, Y
Gravel, D
机构：
[1] Univ Montreal, Dept Chim, Montreal, PQ H3C 3J7, Canada
[2] Inst Rech Clin Montreal, Montreal, PQ H2W 1R7, Canada
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 09期
基金：
加拿大自然科学与工程研究理事会;
关键词：
D O I：
10.1016/S0960-894X(01)00130-5
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The present paper reports the molecular modeling-based design and synthesis of an optically pure noncarbohydrate mimetic of sialyl Lewis X to inhibit E-selectin. Biological evaluation of the designed substance as well as that of its enantiomer gave, contrary to expectations, comparable IC50 values, Results are discussed in terms of receptor binding specificity and the molecular modeling protocol used. (C) 2001 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：1109 / 1112
页数：4
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