Cytotoxicity and Antitumour Activity of Tetrahedral, Bis Diphosphine

5 Cytotoxicity and Antitumour Activity of Tetrahedral, Bis(Diphosphine)Au(I) Complexes 

2 In the clonogenic assay cells are grown on plate surfaces, treated with drugs, washed, then incubated for 5 days in fresh medium. The viability is measured by the ability of a cell to form a colony of greater than 50 cells (see Ref. 54). The IC50 value is the concentration of drug required to reduce the number of colonies formed by 50% relative to controls. 

The differences in the cytotoxic effects of [Au(dppe)2]Cl and auranofin indicate that different mechanisms are involved. The cytotoxic effects of [Au(dppe)2]Cl may be mediated by interference with the reproductive capacity of the cell whereas those produced by auranofin appear to be acutely mediated. An important difference between the two complexes is that the c5dotoxic potency of [Au(dppe)2]Cl is not significantly reduced by the presence of serum proteins in the culture media consistent with the high stability of the complex in the presence of thiols, and in serum  

Tumour model Route of administration dppe [Au(dppe)2]a XAu(dppe)AuX X=C1 X=S (glucose)  

Maximally-tolerated dose for B6D2F mice on an ip. qD x 5 regimen 

---