Parallel solid-phase synthesis of vitronectin receptor (alpha v beta 3) inhibitors

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.