Sialyl Lewisx is one of the natural ligands of E- and P-selectins. Our group showed that Glc-NAc, a polysaccharide subunit that holds in space the fucose and galactose derivative of Sialyl Lewisx, could be advantageously replaced by acyclic tethers possessing a defined conformational bias to provide high levels of E- and P-selectin blocking activity, both in vitro and in vivo. The design and stereoselective synthesis of these molecules, and other analogues thereof, will be presented.

Selectin antagonists: Acyclic tethers with a define conformational bias

249th National Meeting (2015)

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