Gold derivatives for the treatment of cancer.
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.
Tiekink
Edward R T
ER
Department of Chemistry, National University of Singapore, Singapore. chmtert@nus.edu.sg
D000818:Animals; D004353:Drug Evaluation, Preclinical; D017612:Gold Compounds / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D006801:Humans; D015394:Molecular Structure; D009369:Neoplasms / Q000188:drug therapy*; D013329:Structure-Activity Relationship
D017612:Gold Compounds