Biphenyls as potent vitronectin receptor antagonists. Part 3: Squaric acid amides

Vitronectin receptor (αVβ3) antagonists have been implicated as a possible new treatment of restenosis following balloon angioplasty. In this work we investigate a series of novel arginine mimetic scaffolds leading to new insight of the αVβ3/ligand interaction. Squaric acid amide 10 is a subnanomolar αVβ3 antagonist with improved potency on human smooth muscle cell migration.

Vitronectin receptor (αVβ3) antagonists have been implicated as a possible new treatment of restenosis following balloon angioplasty. In this work we investigate a series of novel arginine mimetic scaffolds leading to new insight of the αVβ3/ligand interaction. Squaric acid amide 10 is a subnanomolar αVβ3 antagonist with improved potency on human smooth muscle cell migration.Figure optionsDownload as PowerPoint slide