Potent integrin antagonists from a small library of RGD-including cyclic pseudopeptides

Authors
Belvisi, L Bernardi, A Checchia, A Manzoni, L Potenza, D Scolastico, C Castorina, M Cupelli, A Giannini, G Carminati, P Pisano, C
Citation
L. Belvisi et al., Potent integrin antagonists from a small library of RGD-including cyclic pseudopeptides, ORG LETT, 3(7), 2001, pp. 1001-1004
Citations number
19
Categorie Soggetti
Organic Chemistry/Polymer Science
Journal title
ORGANIC LETTERS
ISSN journal
15237060 → ACNP
Volume
3
Issue
7
Year of publication
2001
Pages
1001 - 1004
Database
ISI
SICI code
1523-7060(20010405)3:7<1001:PIAFAS>2.0.ZU;2-Y
Abstract
A small library of cyclic RGD pseudopentapeptides incorporating stereoisome ric 6,5- and 7,5-fused bicyclic lactams was synthesized with the aim of dev eloping active and selective integrin antagonists. The solid-phase synthesi s and activity of these RGD derivatives is described, The approach led to t wo of the most active known inhibitors of alpha (v)beta (3) receptor.