Small constrained non-peptidic mols. 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.
Synthesis and Biological Evaluation of Nonpeptide alpha-v-beta-3/alpha-5-beta-1 Integrin Dual Antagonists containing 5,6-Dihydropyridin-2-one Scaffolds
BENFATTI, FIDES;CARDILLO, GIULIANA;FABBRONI, SERENA;GALZERANO, PATRIZIA;GENTILUCCI, LUCA;JURIS, RICCARDO;TOLOMELLI, ALESSANDRA;BAIULA, MONICA;SPARTÀ, ANTONINO MARIA;SPAMPINATO, SANTI MARIO
2007
Abstract
Small constrained non-peptidic mols. 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.File in questo prodotto:
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