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