SOLID-PHASE SYNTHESIS OF A SELECTIVE ALPHA(V)BETA(3) INTEGRIN ANTAGONIST LIBRARY

Authors
CORBETT JW GRACIANI NR MOUSA SA DEGRADO WF
Citation
Jw. Corbett et al., SOLID-PHASE SYNTHESIS OF A SELECTIVE ALPHA(V)BETA(3) INTEGRIN ANTAGONIST LIBRARY, Bioorganic & medicinal chemistry letters, 7(11), 1997, pp. 1371-1376
Citations number
23
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
11
Year of publication
1997
Pages
1371 - 1376
Database
ISI
SICI code
0960-894X(1997)7:11<1371:SSOASA>2.0.ZU;2-Z
Abstract
Solid-phase synthesis was used to generate a focused RGD peptide mimet ic library in an effort to identify potent and selective alpha(v) beta (3) integrin antagonists. Increased activity was observed for compound s possessing a urea linkage to piperazine, with the most active compou nd (28) exhibiting an IC50 = 1.1 nM in an alpha(v) beta(3) ELISA assay . (C) 1997 The DuPont Merck Pharmaceutical Company. Published by Elsev ier Science Ltd.