Gold complexes antitumor activity

Table 6.4 Cytotoxcitiy and antitumor activity of selected gold complexes on B16 Melanocytes and P388 leukocyte. Adapted from Shaw [17].

Shaw, C.F. Ill, Beery, A. and Stocco, G.C. (1986) Antitumor activity of two binudear gold(I) complexes with bridging dithiolate ligands. Inorganica Chimica Acta, 123, 213-216. 

Mirabelli, C.K., Johnson, R.K. and Hdl, D.T. (1986) Correlation of the in vitro cytotoxic and in vivo antitumor activities of gold(I) coordination complexes./oumal of Medicinal Chemistry, 29, 218-223. 

McKeage, M.J., Maharaj, L. and Berners-Price, S.J. (2002) Mechanisms of cytotoxicity and antitumor activity of gold(I) phosphine complexes the possible role of mitochondria. Coordination Chemistry Reviews, 232, 127—135. 

Exploration of new complexes with useful antimicrobial activities has stimulated extensive development of synthetic chemistry of silver(I) complexes. The incorporation of novel ligands can moderate the physical and chemical properties of complexes. For example, the bis(diphosphine)silver(I) complexes (which are analogues of the bis(diphosphine)gold(l) complexes with promising antitumor activity compromised by their antimitochondrial activity) were examined for antitumor and antimicrobial activity by... 

The most commonly observed gold(I) compound is a linear two-coordinate complex. Three- and four-coordinate complexes, which wiU be discussed here and in the foUowing section, are substantially less common. Several examples " of three-coordinate complexes are known, some with monodentate phosphine and some with bidentate phosphine ligands. The observation that these complexes have significant antitumor activity has increased interest in these species . The purpose of this work is to calculate the structures of complexes with Au+ bonded to three neutral ligands in order to compare it to the other types of gold(l) complexes discussed above. 

Many gold phosphine complexes have been found to be potent cytotoxic agents, to have antitumor activity against P388 leukaemia and to be active against a spectrum of transplantable tumour models . It has been of particular interest to obtain some of them labeUed with radioactive isotopes of gold and carbon for cellular, binding, metabolism and biodistribution studies. 

Source From Correlation of the in vitro cytotoxic and in vivo antitumor activities of gold(I) coordination complexes,... 

Role of lipophilicity in determining the cellular uptake and antitumor activity of gold phosphine complexes, M. J. McKeage, S. J. Bemers-Price, P. GaUetis, et al., Cancer Chemother. Pharmacol., 2000,46, 343. 

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