Beta-C-mannosides as selectin inhibitors

J Med Chem. 2002 Apr 11;45(8):1563-6. doi: 10.1021/jm010390f.


Potential E- and P-selectin inhibitors were synthesized to explore a hydrophobic area on the E-selectin surface and the PSGL-1 protein binding site on the P-selectin surface that was recently defined by crystallography. Three series of mannose-based compounds (libraries A, B, and C) were synthesized using solution phase parallel synthesis. Biological evaluation of these compounds was done using two ELISA-based assays and transferred NOE (trNOE) experiments. Some of the compounds showed better activity than sLe(x) in the P-selectin assay.

Publication types

  • Comparative Study

MeSH terms

  • Combinatorial Chemistry Techniques
  • Crystallography, X-Ray
  • E-Selectin / chemistry*
  • Enzyme-Linked Immunosorbent Assay
  • Humans
  • Ligands
  • Magnetic Resonance Spectroscopy
  • Mannosides / chemical synthesis*
  • Mannosides / chemistry
  • Membrane Glycoproteins / chemistry
  • Models, Molecular
  • Oligosaccharides / chemistry
  • P-Selectin / chemistry*
  • Protein Binding
  • Sialyl Lewis X Antigen
  • Structure-Activity Relationship


  • E-Selectin
  • Ligands
  • Mannosides
  • Membrane Glycoproteins
  • Oligosaccharides
  • P-Selectin
  • P-selectin ligand protein
  • Sialyl Lewis X Antigen