Phosphine-Gold(I) compounds as anticancer agents: general description and mechanisms of action

João Carlos Lima, Laura Rodríguez

Research output: Contribution to journalReview articlepeer-review

73 Citations (Scopus)

Abstract

Gold complexes have been explored as metallodrugs with great potential applications as antitumoral agents. In particular, gold-phosphine derivatives seemed quite promising since the use of the antiarthritic auranofin drug (thiolate-Au-PEt 3 complex) presented also biological activity against different cancer cells. So, different auranofin analogues have been explored within this context and for this reason, the main number of phosphine-gold complexes developed with this goal contain thiolate ligands. Other complexes have been also studied such as tetrahedral bis(phosphine)gold(I) and phosphine-gold-halides. Very recently, phosphine-gold-alkynyl complexes have also shown very interesting biological activities although few reports are published related to them. Their mechanism of action seems to be clearly different that the used by platinum drugs (DNA intercalating processes) and recent studies point to be related to the inhibition of Trx reductase. Cellular uptake and biodistribution studies are well reported in the original works but the use of luminescence techniques is relatively less explored. For this, the use of these techniques is also specifically reported in this review.

Original languageEnglish
Pages (from-to)921-928
Number of pages8
JournalAnti-Cancer Agents In Medicinal Chemistry
Volume11
Issue number10
Publication statusPublished - 1 Dec 2011

Keywords

  • Anticancer
  • Fluorescence
  • Gold(I)
  • Mechanism
  • Metallodrugs
  • Phosphine
  • Thioredoxin

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