Structure-activity relationship of a series of non peptidic RGD integrin antagonists targeting α5β1: part 1

Bioorg Med Chem Lett. 2012 Jun 15;22(12):4111-6. doi: 10.1016/j.bmcl.2012.04.063. Epub 2012 Apr 21.

Abstract

Potent antagonists of the integrin α(5)β(1), which are RGD mimetics built from tyrosine are described. This letter describes the optimization of in vitro potency obtained by variation of two parts of the molecule, the basic group and the linker between the basic group and the phenyl central core.

MeSH terms

  • Cell Adhesion / drug effects
  • Cell Survival / drug effects
  • Fibrinogen / chemistry
  • Fibronectins / chemistry
  • Humans
  • Integrin alpha5beta1 / antagonists & inhibitors*
  • Integrin alpha5beta1 / metabolism
  • K562 Cells
  • Models, Molecular
  • Molecular Mimicry
  • Oligopeptides / chemical synthesis*
  • Oligopeptides / pharmacology
  • Serum Albumin / chemistry
  • Structure-Activity Relationship
  • Tyrosine / analogs & derivatives*
  • Tyrosine / chemical synthesis*
  • Tyrosine / pharmacology

Substances

  • Fibronectins
  • Integrin alpha5beta1
  • Oligopeptides
  • Serum Albumin
  • Tyrosine
  • arginyl-glycyl-aspartic acid
  • Fibrinogen