Synthesis and antithrombotic activity of carbolinecarboxyl RGD sequence

Bioorg Med Chem Lett. 2002 Feb 25;12(4):585-7. doi: 10.1016/s0960-894x(01)00809-5.

Abstract

3S-1,2,3,4-tetrahydro-beta-carboline-3-carboxylic acid, RGDS, RGDV, RGDF and their linkers were synthesized. The anti-aggregation and adhesion of platelet indicated that the in vitro activities of the linkers remained at the same level as RGDS, RGDV, and RGDF (p>0.05). The antithrombotic activities in vivo suggested, however, that the potencies of RGDS, RGDV and RGDF were enhanced by the introduction of 3S-1,2,3,4-tetrahydro-beta-carboline-3-carboxyl group into their alpha amino group (p<0.05, 0.01 or 0.001).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Carbolines / administration & dosage
  • Carbolines / chemical synthesis*
  • Carbolines / pharmacology
  • Cell Adhesion / drug effects
  • Disease Models, Animal
  • Fibrinolytic Agents / administration & dosage
  • Fibrinolytic Agents / chemical synthesis*
  • Fibrinolytic Agents / pharmacology
  • Humans
  • Male
  • Oligopeptides / administration & dosage
  • Oligopeptides / chemical synthesis*
  • Oligopeptides / pharmacology
  • Platelet Aggregation / drug effects
  • Rabbits
  • Rats
  • Rats, Wistar
  • Structure-Activity Relationship
  • Thrombosis / drug therapy
  • Tumor Cells, Cultured / drug effects

Substances

  • Carbolines
  • Fibrinolytic Agents
  • Oligopeptides
  • arginyl-glycyl-aspartic acid