Gold derivatives for the treatment of cancer

Abstract

The cytotoxicity and anti-tumour activity screening trials for both gold(I) and gold(III) are summarised. Gold(I) thiolates employed clinically in the treatment of rheumatoid arthritis display some potency against various tumours but a greater potential is found in their analogues. In particular, analogues featuring a linear P-Au-S arrangement in which the thiolate ligand is derived from a biologically active thiol display high potency. Further, targeting mitochondria with tetrahedrally coordinated gold(I) phosphine compounds with enhanced hydrophilicity is a research direction with exciting potential. Recent research has shown that gold(III) compounds featuring square-planar geometries, as found in cisplatin, may target DNA and may provide new anti-tumour agents. © 2002 Elsevier Science Ireland Ltd. All rights reserved.