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

Lucas, Stephanie. J., Lord, Rianne M., Basri, Aida M., Allison, Simon J., Phillips, Roger M., Blacker, A. John and McGowan, Patrick C. (2016) Increasing anti-cancer activity with longer tether lengths of group 9 Cp* complexes. Dalton Transactions (16). ISSN 1477-9226

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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.

Item Type: Article
Subjects: Q Science > Q Science (General)
Q Science > QD Chemistry
R Medicine > RS Pharmacy and materia medica
Schools: School of Applied Sciences
Related URLs:
Depositing User: Elizabeth Boulton
Date Deposited: 01 Mar 2016 12:47
Last Modified: 21 Jun 2016 14:02


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