Synthesis and evaluation of graveoline and graveolinine derivatives with potent anti-angiogenesis activities

Eur J Med Chem. 2010 Sep;45(9):3895-903. doi: 10.1016/j.ejmech.2010.05.043. Epub 2010 May 26.

Abstract

A series of graveoline and graveolinine derivatives were synthesized. The biological results showed that most of graveoline derivatives possessed higher cytotoxicity and better inhibitive effect against the adhesion and migration of human umbilical vein endothelial cell (HUVEC) than graveolinine derivatives. Among these compounds, 8d was the most potent agents that also showed significant anti-angiogenesis activities in chick embryo chorioallantoic membrane (CAM) assay.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Angiogenesis Inhibitors / chemical synthesis
  • Angiogenesis Inhibitors / chemistry*
  • Angiogenesis Inhibitors / pharmacology*
  • Angiogenesis Inhibitors / toxicity
  • Animals
  • Cell Adhesion / drug effects
  • Cell Line, Tumor
  • Cell Movement / drug effects
  • Chick Embryo
  • Chorioallantoic Membrane / drug effects
  • Endothelial Cells / cytology
  • Endothelial Cells / drug effects
  • Humans
  • Methoxsalen / analogs & derivatives*
  • Methoxsalen / chemical synthesis
  • Methoxsalen / chemistry
  • Methoxsalen / pharmacology
  • Methoxsalen / toxicity
  • Quinolones / chemical synthesis
  • Quinolones / pharmacology*
  • Quinolones / toxicity

Substances

  • Angiogenesis Inhibitors
  • Quinolones
  • graveoline
  • Methoxsalen