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Potent integrin antagonists from a small library of RGD-including cyclic pseudopeptides
L Belvisi1, A Bernardi, A Checchia
1Dipartimento di Chimica Organica e Industriale, Università degli Studi di Milano, via Venezian 21, I-20133 Milano, Italy.
Organic Letters
|March 30, 2001
Abstract:
[structure: see text]. 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 alpha(V)beta3 receptor.