Parallel solid-phase synthesis of vitronectin receptor (alphavbeta3) inhibitors.
A combinatorial approach for rapid optimization of a vitronectin receptor (alphavbeta3) inhibitor lead was accomplished by solid-phase synthesis. Orthogonally bis protected 2,3-diaminopropionic acid was used to immobilize the C-terminus of the molecule. Selective deprotection and functionalization of the alpha-amino group followed by acyl resorcinol scaffold attachment and N-terminus diversification was used to explore structure activity relationship (SAR).
Wyeth-Ayerst Research, Pearl River, NY 10965, USA. gopalsa@war.wyeth.com
A
A
Gopalsamy
H
H
Yang
J W
JW
Ellingboe
K L
KL
Kees
J
J
Yoon
R
R
Murrills
D019030:Receptors, Vitronectin / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D019030:Receptors, Vitronectin