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.
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.
authors.affiliation: Dipartimento di Chimica "G. Ciamician", Università di Bologna, Via Selmi 2, 40126 Bologna, Italy.
authors.forename: Fides
authors.initials: F
authors.lastname: Benfatti
authors.forename: Giuliana
authors.initials: G
authors.lastname: Cardillo
authors.forename: Serena
authors.initials: S
authors.lastname: Fabbroni
authors.forename: Patrizia
authors.initials: P
authors.lastname: Galzerano
authors.forename: Luca
authors.initials: L
authors.lastname: Gentilucci
authors.forename: Riccardo
authors.initials: R
authors.lastname: Juris
authors.forename: Alessandra
authors.initials: A
authors.lastname: Tolomelli
authors.forename: Monica
authors.initials: M
authors.lastname: Baiula
authors.forename: Antonino
authors.initials: A
authors.lastname: Spartà
authors.forename: Santi
authors.initials: S
authors.lastname: Spampinato
mesh_terms: D002448:Cell Adhesion / Q000187:drug effects; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D039081:Integrin alpha5beta1 / Q000037:antagonists & inhibitors*; D039302:Integrin alphaVbeta3 / Q000037:antagonists & inhibitors*; D020014:K562 Cells; D008024:Ligands; D015394:Molecular Structure; D011725:Pyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011728:Pyridones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D054852:Small Molecule Libraries; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D039081:Integrin alpha5beta1; D039302:Integrin alphaVbeta3; D008024:Ligands; D011725:Pyridines; D011728:Pyridones; D054852:Small Molecule Libraries