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

نویسندگان

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

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 () and iridium () 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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عنوان ژورنال:
  • Dalton transactions

دوره 45 16  شماره 

صفحات  -

تاریخ انتشار 2016