Biphenyls as potent vitronectin receptor antagonists

Vitronectin receptor (α Vβ 3) antagonism has been implicated as a mechanism for the treatment of restenosis following balloon angioplasty. In this work we present results from screening of a focused combinatorial library based on a biphenyl moiety. Our SAR studies led to the identification of compou...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2002-01, Vol.12 (2), p.205-208
Hauptverfasser:	Urbahns, Klaus, Härter, Michael, Albers, Markus, Schmidt, Delf, Stelte-Ludwig, Beatrix, Brüggemeier, Ulf, Vaupel, Andrea, Gerdes, Christoph
Format:	Artikel
Sprache:	eng
Schlagworte:	Biological and medical sciences Biphenyl Compounds - chemistry Biphenyl Compounds - pharmacology Combinatorial Chemistry Techniques Hypnotics. Sedatives Medical sciences Neuropharmacology Pharmacology. Drug treatments Psychology. Psychoanalysis. Psychiatry Psychopharmacology Receptors, Vitronectin - antagonists & inhibitors Structure-Activity Relationship
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Zusammenfassung:	Vitronectin receptor (α Vβ 3) antagonism has been implicated as a mechanism for the treatment of restenosis following balloon angioplasty. In this work we present results from screening of a focused combinatorial library based on a biphenyl moiety. Our SAR studies led to the identification of compounds with subnanomolar activity, selectivity towards the related GPIIbIIIa receptor and functional activity on human smooth muscle cell migration. Identified from a combinatorial library based on a biphenyl moiety, 30 is a subnanomolar vitronectin receptor (α Vβ 3) antagonist with selectivity towards the related GPIIbIIIa receptor and functional activity on human smooth muscle cell migration.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(01)00717-X