(matrix presented) 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.
Potent integrin antagonists from a small library of RGD-including cyclic pseudopeptides / L. Belvisi, A. Bernardi, A. Checchia, L. Manzoni, D. Potenza, C. Scolastico, M. Castorina, A. Cupelli, G. Giannini, P. Carminati, C. Pisano. - In: ORGANIC LETTERS. - ISSN 1523-7060. - 3:7(2001), pp. 1001-1004. [10.1021/ol007049u]
Potent integrin antagonists from a small library of RGD-including cyclic pseudopeptides
L. BelvisiPrimo
;A. BernardiSecondo
;L. Manzoni;D. Potenza;C. Scolastico;
2001
Abstract
(matrix presented) 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.
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