Analyses of Titanocenes in the spheroid-based cellular angiogenesis assay.
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.
Weber
Holger
H
ProQinase GmbH Freiburg, Breisacher Str. 117, D-79106 Freiburg, Germany.
Claffey
James
J
Hogan
Megan
M
Pampillón
Clara
C
Tacke
Matthias
M
D020533:Angiogenesis Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D002478:Cells, Cultured; D042783:Endothelial Cells / Q000187:drug effects* / Q000648:ultrastructure; D004730:Endothelium, Vascular / Q000166:cytology / Q000187:drug effects / Q000254:growth & development; D006801:Humans; D018374:LLC-PK1 Cells; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013552:Swine
D020533:Angiogenesis Inhibitors; D009942:Organometallic Compounds; C406884:titanocene