Synthesis and anti-angiogenic activity of cortistatin analogs

Biosci Biotechnol Biochem. 2008 Nov;72(11):2992-7. doi: 10.1271/bbb.80562. Epub 2008 Nov 7.

Abstract

Analogs of cortistatins, a series of anti-angiogenic compounds isolated from the Indonesian marine sponge Cortisium simplex, were synthesized from estrone by using the Suzuki-Miyaura coupling reaction as the key step. The estrone-isoquinoline hybridized compound showed selective inhibitory activity against the proliferation and VEGF-induced migration of HUVEC.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Angiogenesis Inhibitors / chemical synthesis*
  • Angiogenesis Inhibitors / chemistry
  • Angiogenesis Inhibitors / pharmacology*
  • Animals
  • Cell Line
  • Cell Movement / drug effects
  • Cell Proliferation / drug effects
  • Endothelial Cells / cytology
  • Endothelial Cells / drug effects
  • Estrone / analogs & derivatives
  • Humans
  • Mice
  • Neuropeptides / chemical synthesis*
  • Neuropeptides / chemistry
  • Neuropeptides / pharmacology*
  • Vascular Endothelial Growth Factor A / pharmacology

Substances

  • Angiogenesis Inhibitors
  • Neuropeptides
  • Vascular Endothelial Growth Factor A
  • cortistatin
  • Estrone