A combinatorial approach for rapid optimization of a vitronectin receptor (
alpha v beta 3) inhibitor lead was accomplished by solid-phase synthesis. O
rthogonally bis protected 2,3-diaminopropionic acid was used to immobilize
the C-terminus of the molecule. Selective deprotection and functionalizatio
n of the alpha-amino group followed by acyl resorcinol scaffold attachment
and N-terminus diversification was used to explore structure-activity relat
ionship (SAR). (C) 2000 Elsevier Science Ltd. All rights reserved.