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

Stephanie J. Lucas, Rianne M. Lord, Aida M. Basri, Simon J. Allison, Roger M. Phillips, A. John Blacker, Patrick C. McGowan

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29 Citations (Scopus)

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.
Original languageEnglish
Pages (from-to)6812-6815
Number of pages4
JournalDalton Transactions
Volume45
Issue number16
DOIs
Publication statusPublished - 17 Feb 2016

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