Tuning the hydrophobicity of ruthenium(II)–arene (RAPTA) drugs to modify uptake, biomolecular interactions and efficacy

Claudine Scolaro; Adrian B. Chaplin; Christian G. Hartinger; Alberta Bergamo; Moreno Cocchietto; Bernhard K. Keppler; Gianni Sava; Paul J. Dyson

doi:10.1039/B705449A

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Dalton Transactions

Issue 43, 2007

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Tuning the hydrophobicity of ruthenium(II)–arene (RAPTA) drugs to modify uptake, biomolecular interactions and efficacy

Claudine Scolaro , Adrian B. Chaplin , Christian G. Hartinger , Alberta Bergamo , Moreno Cocchietto , Bernhard K. Keppler , Gianni Sava and Paul J. Dyson

Dalton Trans., 2007, 5065-5072

DOI: 10.1039/B705449A
Received 12 Apr 2007, Accepted 22 May 2007
First published on the web 26 Sep 2007
This article is part of the collection: Dalton Discussion 10: Applications of metals in medicine and healthcare

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The antitumour activity of the organometallic ruthenium(II)–arene mixed phosphine complexes, [Ru(η⁶-p-cymene)Cl(PTA)(PPh₃)]BF₄1b and [Ru(η⁶-C₆H₅CH₂CH₂OH)Cl(PTA)(PPh₃)]BF₄2b (PTA = 1,3,5-triaza-7-phosphaadamantane), have been evaluated in vitro and compared to their RAPTA analogues, [Ru(η⁶-p-cymene)Cl₂(PTA)] 1a and [Ru(η⁶-C₆H₅CH₂CH₂OH)Cl₂(PTA)] 2a. The results show that the addition of the PPh₃ ligand to 2a increases the cytotoxicity towards the TS/A adenocarcinoma cancer cells, which correlates with increased uptake, but also increases cytotoxicity to non-tumourigenic HBL-100 cells, thus decreasing selectivity. The decrease in selectivity has been correlated to increased DNA interactions relative to proteins, demonstrated by reactivity of the compounds with a 14-mer oligonucleotide and the model proteins ubiquitin and cytochrome-c.

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Claudine Scolaro
Adrian B. Chaplin
Christian G. Hartinger
Alberta Bergamo
Moreno Cocchietto
Bernhard K. Keppler
Gianni Sava
Paul J. Dyson

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Dalton Transactions

Tuning the hydrophobicity of ruthenium(II)–arene (RAPTA) drugs to modify uptake, biomolecular interactions and efficacy

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