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Biphenyls as potent vitronectin receptor antagonists. Part 3: Squaric acid amides
Klaus Urbahns1, Michael Härter, Markus Albers
1Institute of Medicinal Chemistry, Bayer Healthcare AG, Bayer-Schering Pharma, 42096 Wuppertal, Germany. Klaus.Urbahns@astrazeneca.com
Abstract:
Vitronectin receptor (alpha(V)beta(3)) 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 alpha(V)beta(3)/ligand interaction. Squaric acid amide 10 is a subnanomolar alpha(V)beta(3) antagonist with improved potency on human smooth muscle cell migration.
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