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Anti-Cancer Agents in Medicinal Chemistry


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

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

Author(s): Joao Carlos Lima and Laura Rodriguez

Volume 11, Issue 10, 2011

Page: [921 - 928] Pages: 8

DOI: 10.2174/187152011797927670

Price: $65


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.

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

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