Analyses of Titanocenes in the spheroid-based cellular angiogenesis assay

Toxicol In Vitro. 2008 Mar;22(2):531-4. doi: 10.1016/j.tiv.2007.09.014. Epub 2007 Sep 29.

Abstract

Titanocene dichloride and two of its derivatives (Titanocene Y and C) were tested on human umbilical vein endothelial cells (HUVEC) sprouting in a spheroid-based cellular angiogenesis assay in order to determine IC50 values of inhibition. Titanocene dichloride and Titanocene Y inhibited HUVEC sprouting in this angiogenesis assay with IC50 values of 19 microM and 4.9 microM, while Titanocene C surprisingly showed no inhibition. This classifies Titanocene dichloride as a purely anti-angiogenic anticancer drug and Titanocene C as a purely cytotoxic anticancer drug. On the other hand, Titanocene Y combines both favourable anticancer activities and seems to be the drug candidate of choice for further optimisation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Angiogenesis Inhibitors / chemical synthesis
  • Angiogenesis Inhibitors / chemistry
  • Angiogenesis Inhibitors / pharmacology*
  • Animals
  • Cells, Cultured
  • Endothelial Cells / drug effects*
  • Endothelial Cells / ultrastructure
  • Endothelium, Vascular / cytology
  • Endothelium, Vascular / drug effects
  • Endothelium, Vascular / growth & development
  • Humans
  • LLC-PK1 Cells
  • Organometallic Compounds / chemical synthesis
  • Organometallic Compounds / chemistry
  • Organometallic Compounds / pharmacology*
  • Swine

Substances

  • Angiogenesis Inhibitors
  • Organometallic Compounds
  • titanocene