Synthesis, cellular uptake and biological activity against pathogenic microorganisms and cancer cells of rhodium and iridium N-heterocyclic carbene complexes bearing charged substituents
MetadataShow full item record
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.
Showing items related by title, author, creator and subject.
Methylation of Ir(III)-tetrazolato complexes: An effective route to modulate the emission outputs and to switch to antimicrobial propertiesFiorini, V.; Zanoni, I.; Zacchini, S.; Costa, A.; Hochkoeppler, A.; Zanotti, V.; Ranieri, Anna; Massi, Massimiliano; Stefan, A.; Stagni, S. (2017)Two neutral cyclometalated Ir(iii)-tetrazolato complexes that differ by variations of the substituents on either the phenylpyridine or the tetrazolate ligand have been converted into the corresponding methylated and ...
Morgan, Dale (2007)Bacterial resistance to non-antibiotic agents is being increasingly studied. Plasmid-mediated resistance to cationic agents, which are important biocides, has been described in antibiotic-resistant Staphylococcus aureus. ...
Delineation of Natural and Anthropogenic Process Controlling Hydrogeochemistry of Layered Aquifer SequenceThilagavathi, R.; Chidambaram, S.; Thivya, C.; Prasanna, Mohan Viswanathan; Singaraja, C.; Tirumalesh, K.; Pethaperumal, S. (2014)Groundwater is the source for many activities in urban regions and the quality plays a significant role in determination of its usage. In coastal regions the situation becomes more complex due to the interplay of complex ...