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Issue 16, 2016
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Increasing anti-cancer activity with longer tether lengths of group 9 Cp* complexes

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Abstract

Here in, we report the cytotoxicity of both rhodium and iridium functionalised Cp* analogues of the [Cp*MCl2]2 dimers. The functionalised dimers contain a hydroxy tethered arm of differing carbon length. These show promising IC50 values when tested against HT-29, A2780 and cisplatin-resistant A2780cis human cancer cell lines, with the cytotoxicity improving proportionally with an increase in carbon tether length of the Cp* ring. The most promising results are seen for the 14-carbon Cp* tethered rhodium (2d) and iridium (3b) complexes, which show up to a 24-fold increase in IC50 compared to the unfunctionalised [Cp*MCl2]2 dimer. All complexes were potent inhibitors of purified thioredoxin reductase suggesting that disruption of cellular anti-oxidant function is one potential mechanism of action.

Graphical abstract: Increasing anti-cancer activity with longer tether lengths of group 9 Cp* complexes

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Publication details

The article was received on 14 Jan 2016, accepted on 16 Feb 2016 and first published on 17 Feb 2016


Article type: Communication
DOI: 10.1039/C6DT00186F
Citation: Dalton Trans., 2016,45, 6812-6815
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    Increasing anti-cancer activity with longer tether lengths of group 9 Cp* complexes

    Stephanie. J. Lucas, R. M. Lord, A. M. Basri, S. J. Allison, R. M. Phillips, A. J. Blacker and P. C. McGowan, Dalton Trans., 2016, 45, 6812
    DOI: 10.1039/C6DT00186F

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