Antiangiogenic versus cytotoxic activity in analogues of aeroplysinin-1

Bioorg Med Chem. 2007 Aug 1;15(15):5300-15. doi: 10.1016/j.bmc.2007.05.011. Epub 2007 May 6.

Abstract

A series of analogues of the potentially angiogenic inhibitor aeroplysinin-1 1 were synthesized and their in vitro antiangiogenic and cytotoxic activities evaluated. In the case of epoxy ketone 6 and azlactone 36 the relationship sprouting inhibition assay/cytotoxicity in BAE cells was enhanced by one order and two orders of magnitude, respectively, with respect to the reference. These results imply more specific antiangiogenic properties for the synthesized derivatives.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetonitriles / chemistry*
  • Acetonitriles / pharmacology*
  • Animals
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology*
  • Cattle
  • Cells, Cultured
  • Cyclohexenes / chemistry*
  • Cyclohexenes / pharmacology*
  • Endothelial Cells / cytology
  • Endothelial Cells / drug effects*
  • Endothelial Cells / metabolism
  • Inhibitory Concentration 50
  • Molecular Conformation
  • Neovascularization, Physiologic / drug effects*
  • Structure-Activity Relationship

Substances

  • Acetonitriles
  • Antineoplastic Agents
  • Cyclohexenes
  • aeroplysinin I