Abstract:
A series of new neutral mononuclear or dinuclear gold(I) complexes and a cyclic cationic
tetranuclear amidogold(I) complex comprising of the phosphines 1,2-
bis(dimethylphosphino)ethane (dmpe), μ-1,2–bis(diphenylphosphino)ethane (dppe), μ-1,3-
bis(diphenylphosphino)propane (dppp), μ-1,5-bis(diphenylphosphino)pentane (dpppe), μ-1,6-
bis(diphenylphosphino)hexane (dpph) or trimethylphosphine, and several N-heterocyclic ring
systems (imidazolate, pyrazolate, 1,2,3-triazolate, 1,2,4-triazolate, pyrrolate, 9H-purine-9-ate or
9H-purine-6-amine-9-ate) as ligands, reveal intermolecular aurophilic interactions and 2D
channels available for solvent molecules in some of their crystal structures. The antitumour activity of the acyclic gold(I) compounds is highly dependent on the substituents on the
phosphorus atoms being highest for phenyl groups and lower for methyl groups. The activity of
these compounds against selected cell lines is linked to the length of the carbon bridge between
the two phosphorus atoms being highest with a bridge consisting of 5 or 6 carbons. Two
compounds with the highest tumour specifities that contain dpppe and pyrazolate (a lipophilic
compound) or 1,2,4-triazolate (a hydrophilic compound) induce the apoptic cell death pathway
and tolerate a maximum dose of 1.5 μmol/kg when administered to Balb/C mice.
