Chemical biology of anticancer gold(III) and gold(I) complexes

Chem Soc Rev. 2015 Dec 21;44(24):8786-801. doi: 10.1039/c5cs00132c. Epub 2015 Apr 14.

Abstract

Gold complexes have recently gained increasing attention in the design of new metal-based anticancer therapeutics. Gold(III) complexes are generally reactive/unstable under physiological conditions via intracellular redox reactions, and the intracellular Au(III) to Au(I) reduction reaction has recently been "traced" by the introduction of appropriate fluorescent ligands. Similar to most Au(I) complexes, Au(III) complexes can inhibit the activities of thiol-containing enzymes, including thioredoxin reductase, via ligand exchange reactions to form Au-S(Se) bonds. Nonetheless, there are examples of physiologically stable Au(III) and Au(I) complexes, such as [Au(TPP)]Cl (H2TPP = 5,10,15,20-tetraphenylporphyrin) and [Au(dppe)2]Cl (dppe = 1,2-bis(diphenylphosphanyl)ethane), which are known to display highly potent in vitro and in vivo anticancer activities. In this review, we summarize our current understanding of anticancer gold complexes, including their mechanisms of action and the approaches adopted to improve their anticancer efficiency. Some recent examples of gold anticancer chemotherapeutics are highlighted.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Humans
  • Molecular Structure
  • Neoplasms / drug therapy*
  • Neoplasms / pathology
  • Organogold Compounds / chemistry*
  • Organogold Compounds / pharmacology*

Substances

  • Antineoplastic Agents
  • Organogold Compounds