Synthesis and biological evaluation of vitamin K derivatives as angiogenesis inhibitor

Bioorg Med Chem. 2010 Sep 1;18(17):6305-9. doi: 10.1016/j.bmc.2010.07.022. Epub 2010 Jul 13.

Abstract

Ten vitamin K(3) derivatives were synthesized and screened for anti-angiogenic activity. Results indicated that amine derivatives (1a-d) exerted a stronger inhibition effect on angiogenesis compared to alkyl derivatives (2a-d). In addition to being the most potent inhibitor, 1b also suppressed human umbilical vein endothelial cell tube formation and proliferation. These results suggest that vitamin K(3) amine derivatives with shorter alkyl chains, such as 1b, could be useful for developing anti-angiogenic agents.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Angiogenesis Inhibitors / chemical synthesis*
  • Angiogenesis Inhibitors / pharmacology*
  • Animals
  • Aorta / cytology
  • Aorta / drug effects
  • Cell Proliferation / drug effects
  • Cells, Cultured
  • Endothelial Cells / drug effects
  • Humans
  • Male
  • Rats
  • Rats, Wistar
  • Vitamin K 3 / analogs & derivatives*
  • Vitamin K 3 / chemical synthesis
  • Vitamin K 3 / pharmacology*

Substances

  • Angiogenesis Inhibitors
  • Vitamin K 3