Biphenyls as potent vitronectin receptor antagonists

Bioorg Med Chem Lett. 2002 Jan 21;12(2):205-8. doi: 10.1016/s0960-894x(01)00717-x.

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.

MeSH terms

  • Biphenyl Compounds / chemistry
  • Biphenyl Compounds / pharmacology*
  • Combinatorial Chemistry Techniques
  • Receptors, Vitronectin / antagonists & inhibitors*
  • Structure-Activity Relationship

Substances

  • Biphenyl Compounds
  • Receptors, Vitronectin