Journal
EUROPEAN JOURNAL OF INORGANIC CHEMISTRY
Volume 2013, Issue 32, Pages 5547-5554Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ejic.201300820
Keywords
Bioinorganic chemistry; Biological activity; Medicinal chemistry; Antitumor agents; Antibiotics; Carbene complexes; Rhodium; Iridium
Categories
Funding
- Alexander-von-Humboldt Foundation
- Fonds der Chemischen Industrie (FCI)
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Four new N-heterocyclic carbene (NHC) rhodium and iridium complexes decorated with anionic or cationic pendant groups to increase their water solubility and biological activity have been synthesised and characterised. The lipophilicity of the complexes was determined and the complexes that contained cationic phosphonium groups can be considered delocalised lipophilic cations (DLCs). All complexes were tested for their antibacterial, antiparasitic and anticancer activity, with only the phosphonium-functionalised complexes showing moderate to high activity, whereas the exchange of metal from rhodium to iridium had a negligible effect. Most promising was the activity on Trypanosoma brucei, with IC50 values in the range of 150-400 nM and a selectivity index (SI) of up to 50. General toxicity on mammalian cell lines was a general problem, though, and needs to be mitigated in future work. Cellular uptake studies clearly confirmed that the cationic phosphonium groups facilitated uptake, which was linked with higher biological activity.
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