203794-76-7Relevant academic research and scientific papers
Synthesis and biological evaluation of a sialyl Lewis X mimic with significantly improved E-selectin inhibition
Thoma, Gebhard,Magnani, John L.,Patton, John T.
, p. 923 - 925 (2007/10/03)
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.
