Phosphine-Gold(I) Compounds as Anticancer Agents: General Description and Mechanisms of Action

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)

Volume 17, 14 Issues, 2017

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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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  • 27th of 59 in Chemistry, Medicinal

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Michelle Prudhomme
Institut de Chimie de Clermont-Ferrand
Université Clermont Auvergne

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Phosphine-Gold(I) Compounds as Anticancer Agents: General Description and Mechanisms of Action

Anti-Cancer Agents in Medicinal Chemistry, 11(10): 921-928.

Author(s): Joao Carlos Lima and Laura Rodriguez.

Affiliation: REQUIMTE, Departamento de Quimica, Centro de Quimica Fina e Biotecnologia, Universidade Nova de Lisboa, Quinta da Torre, 2825 Monte de Caparica, Portugal.


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-PEt3 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.


lipophilicity, toxicity, lipophilic-cationic complexes, Gold(I), anticancer, phosphine, fluorescence, mechanism, thioredoxin, metallodrugs.

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Article Details

Volume: 11
Issue Number: 10
First Page: 921
Last Page: 928
Page Count: 8
DOI: 10.2174/187152011797927670
Price: $58

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