4.6 Review

Gold derivatives for the treatment of cancer

Journal

CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY
Volume 42, Issue 3, Pages 225-248

Publisher

ELSEVIER SCIENCE INC
DOI: 10.1016/S1040-8428(01)00216-5

Keywords

gold(I); gold(III); thiolates; phosphines; cancer; rheumatoid arthritis

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The cytotoxicity and anti-tumour activity screening trials for both gold(I) and gold(III) are summarised. Gold(l) 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. (C) 2002 Elsevier Science Ireland Ltd. All rights reserved.

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