Parallel solid-phase synthesis of vitronectin receptor (αvβ3) inhibitors

A Gopalsamy, H Yang, JW Ellingboe, KL Kees…

Index: Gopalsamy, Ariamala; Yang, Hui; Ellingboe, John W.; Kees, Kenneth L.; Yoon, Jeanne; Murrills, Richard Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 15 p. 1715 - 1718

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Citation Number: 13

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 ...