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Increasing anti-cancer activity with longer tether lengths of group 9 Cp* complexes
Lucas, S.J. Lord, Rianne M. Basri, A.M. Allison, Simon J. Phillips, Roger M. Blacker, A.J. McGowan, P.C.
Lucas, S.J.
Lord, Rianne M.
Basri, A.M.
Allison, Simon J.
Phillips, Roger M.
Blacker, A.J.
McGowan, P.C.
Publication Date
2016-04
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© 2016 RSC. Reproduced with permission from the publisher in accordance with the publisher's self-archiving policy.
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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.
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Lucas SJ, Lord RM, Basri AM, Allison SJ, Phillips RM, Blacker AJ and McGowan PC (2016) Increasing anti-cancer activity with longer tether lengths of group 9 Cp* complexes [Communication]. Dalton Transactions. 45(16): 6812.
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