Potent Integrin Antagonists from a Small Library of RGD-Including Cyclic Pseudopeptides

A small library of cyclic RGD pseudopentapeptides incorporating stereoisomeric 6,5- and 7,5-fused bicyclic lactams was synthesized with the aim of developing active and selective integrin antagonists. The solid-phase synthesis and activity of these RGD derivatives is described. The approach led to t...

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Veröffentlicht in:	Organic letters 2001-04, Vol.3 (7), p.1001-1004
Hauptverfasser:	Belvisi, Laura, Bernardi, Anna, Checchia, Anna, Manzoni, Leonardo, Potenza, Donatella, Scolastico, Carlo, Castorina, Massimo, Cupelli, Amelia, Giannini, Giuseppe, Carminati, Paolo, Pisano, Claudio
Format:	Artikel
Sprache:	eng
Schlagworte:	Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - metabolism Bridged Bicyclo Compounds - chemical synthesis Bridged Bicyclo Compounds - chemistry Bridged Bicyclo Compounds - metabolism Cyclization Kinetics Lactams - chemical synthesis Lactams - chemistry Lactams - metabolism Molecular Structure Oligopeptides - chemical synthesis Oligopeptides - chemistry Oligopeptides - metabolism Peptide Library Peptides - metabolism Platelet Aggregation Inhibitors - metabolism Protein Structure, Secondary Radioligand Assay Receptors, Vitronectin - antagonists & inhibitors Receptors, Vitronectin - chemistry
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Zusammenfassung:	A small library of cyclic RGD pseudopentapeptides incorporating stereoisomeric 6,5- and 7,5-fused bicyclic lactams was synthesized with the aim of developing active and selective integrin antagonists. The solid-phase synthesis and activity of these RGD derivatives is described. The approach led to two of the most active known inhibitors of αVβ3 receptor.
ISSN:	1523-7060 1523-7052
DOI:	10.1021/ol007049u