Horvath, Ulrike E.I.Dobrzanska, LilianaStrasser, Christoph E.Bouwer, WilnaJoone, Gisela KätheJansen van Rensburg, Constance ElizabethCronje, StephanieRaubenheimer, Helgard G.2012-05-232012-05-232012-06Ulrike E.I. Horvath, Liliana Dobrzańska, Christoph E. Strasser, Wilna Bouwer, Gisela Joone, Constance E. Jansen van Rensburg, Stephanie Cronje & Helgard G. Raubenheimer, Amides of gold(I) diphosphines prepared from N-heterocyclic sources and their in vitro and in vivo screening for anticancer activity, Journal of Inorganic Biochemistry, vol. 111, no. 6, pp. 80-90 (2012), doi: 10.1016/j.jinorgbio.2012.02.0260162-0134 (print)1872-3344 (online)10.1016/j.jinorgbio.2012.02.026http://hdl.handle.net/2263/18841A 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.en© 2012 Elsevier Inc. All rights reserved.AzolatePurine-ateGold(I) diphosphinesCytotoxicityPyrazolateAnti-tumourPostprint Article