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ID: ALA1137514

Journal: Bioorg Med Chem

Title: Synthesis and biological evaluation of non-peptide alpha(v)beta(3)/alpha(5)beta(1) integrin dual antagonists containing 5,6-dihydropyridin-2-one scaffolds.

Authors: Benfatti F, Cardillo G, Fabbroni S, Galzerano P, Gentilucci L, Juris R, Tolomelli A, Baiula M, Spartà A, Spampinato S.

Abstract: Small constrained non-peptidic molecules consisting of a polyfunctionalized rigid core, carrying appendages corresponding to arginine and aspartic acid side chains, have been recently reported to be promising for drug development. In this work, the 5,6-dihydropyridin-2-one was envisaged as a scaffold to turn into potential integrin ligands, introducing a carboxylic acid and a basic appendage. The synthesis and the antiadhesion activity of a small library of peptidomimetics capable to recognize alpha(v)beta(3) and alpha(5)beta(1) integrins has been herein reported.

CiteXplore: 17869121

DOI: 10.1016/j.bmc.2007.07.049