Drug design, synthesis, and evaluation of a non-sugar-based selectin antagonist

We have designed a series of simple rigid compounds (2) having a phenyl rin g attached to three essential groups necessary for selectin binding, i.e., a fucose unit, a carboxylic acid, and the hydrophobic part. In this series of compound 2, 2a exhibited strong inhibitory activity in in vitro P-select in mediated cell adhesion assay. The novel type of compound 2a would be a p otential lead compound for selectin antagonist. (C) 2001 Elsevier Science L td. All rights reserved.