title: Biphenyls as potent vitronectin receptor antagonists.
abstract: Vitronectin receptor (alpha(V)beta(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.
authors.affiliation: Institute of Medicinal Chemistry, Pharma Research Centre, Bayer AG, D-42096 Wuppertal, FRG. klaus.urbahns.ku1@bayer.co.jp
authors.forename: Klaus
authors.initials: K
authors.lastname: Urbahns
authors.forename: Michael
authors.initials: M
authors.lastname: Härter
authors.forename: Markus
authors.initials: M
authors.lastname: Albers
authors.forename: Delf
authors.initials: D
authors.lastname: Schmidt
authors.forename: Beatrix
authors.initials: B
authors.lastname: Stelte-Ludwig
authors.forename: Ulf
authors.initials: U
authors.lastname: Brüggemeier
authors.forename: Andrea
authors.initials: A
authors.lastname: Vaupel
authors.forename: Christoph
authors.initials: C
authors.lastname: Gerdes
mesh_terms: D001713:Biphenyl Compounds / Q000737:chemistry / Q000494:pharmacology*; D020650:Combinatorial Chemistry Techniques; D019030:Receptors, Vitronectin / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D001713:Biphenyl Compounds; D019030:Receptors, Vitronectin