Title of article
Synthesis and biological evaluation of a sialyl lewis X mimic with significantly improved E-selectin inhibition
Author/Authors
Gebhard Thoma، نويسنده , , John L. Magnani، نويسنده , , John T. Patton، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2001
Pages
3
From page
923
To page
925
Abstract
The synthesis of the highly potent E-selectin inhibitor 5 is described. Sialyl Lewis X mimic 5 was rationally designed by combining two previously disclosed beneficial sLex modifications in a single molecule. The compound was found to be 30-fold more potent than sLex in a static, cell-free equilibrium assay. Furthermore, compound 5 was highly active (IC50=10 μM) in a dynamic non-equilibrium assay in which sLex did not inhibit neutrophil rolling at up to 1000 μM.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2001
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
791307
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