Glutathione activation of an organometallic half-sandwich anticancer drug candidate by ligand attack

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Abstract
In contrast to the clinical drug cisplatin, the anticancer complex [Os(η6-p-cymene)(4-(2-pyridylazo)-N,N-dimethylaniline)I]+ [1-I] is inert towards hydrolysis and targets cancer cell metabolism rather than DNA. A combination of DFT calculations and X-ray absorption spectroscopy (XAS) suggests that hydrolytic activation of 1-I involves catalytic attack by the intracellular tripeptide glutathione (GSH) on the azo bond of the chelating ligand in the complex.
Funding Information
  • Wellcome Trust (107691/Z/15/Z)
  • Cancer Research UK (C53561/A19933)
  • European Synchrotron Radiation Facility (CH-5212)
  • Engineering and Physical Sciences Research Council (EP/F034210/1)

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