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.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Cell Adhesion / drug effects
-
Cell Line, Tumor
-
Drug Screening Assays, Antitumor
-
Humans
-
Integrin alpha5beta1 / antagonists & inhibitors*
-
Integrin alphaVbeta3 / antagonists & inhibitors*
-
K562 Cells
-
Ligands
-
Molecular Structure
-
Pyridines / chemical synthesis*
-
Pyridines / chemistry
-
Pyridines / pharmacology*
-
Pyridones / chemical synthesis*
-
Pyridones / chemistry
-
Pyridones / pharmacology*
-
Small Molecule Libraries
-
Stereoisomerism
-
Structure-Activity Relationship
Substances
-
Integrin alpha5beta1
-
Integrin alphaVbeta3
-
Ligands
-
Pyridines
-
Pyridones
-
Small Molecule Libraries