Author/Authors :
Ariamala Gopalsamy، نويسنده , , Hui Yang، نويسنده , , John W. Ellingboe، نويسنده , , Kenneth L. Kees، نويسنده , , Jeanne Yoon، نويسنده , , Richard Murrills، نويسنده ,
Abstract :
A combinatorial approach for rapid optimization of a vitronectin receptor (αvβ3) 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 α-amino group followed by acyl resorcinol scaffold attachment and N-terminus diversification was used to explore structure–activity relationship (SAR).
