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EnglishWe report the synthesis, characterization, and biological activity of IrIcomplexes with triazole- (NNHC) and thiazole-based (NSHC) N-heterocyclic carbene ligands. Starting from the dimeric [Ir(COD)Cl]2, we obtained complexes of composition Ir(COD)(NNHC)Cl (4a), Ir(COD)(NNHC)X (4b: X = Cl; 4bBr: X = Br), [Ir(COD)(NNHC)(NHC)]I (5a), [Ir(COD)(NSHC)2]Cl (6a), and [Ir(COD)(NSHC)(NNHC)]Cl (6b) by adaptation of established synthetic methods for metal–NHC complexes. Their interactions with model proteins cytochrome c and lysozyme, as well as with the oligonucleotide hexamer (CG)3(ODN1), were studied. Although most complexes did not show any strong interactions with these biomolecules, all complexes were active against HT-29 and MCF-7 cancerous cells, with IC50values ranging between 1 and 60 µm. The most active compounds were the cationic bis(carbene) derivatives 5 and 6. All compounds generated high levels of reactive oxygen species (ROS) after incubation for 48 h in MCF-7 cells, possibly suggesting a redox-mediated mechanism of action. Interestingly, there were distinctive differences in the superoxide/(total ROS) ratios induced by the different groups of compounds.
| Autori interni: | ||
| Autori: | Gothe, Yvonne; Romero-Canelón, Isolda; Marzo, Tiziano; Sadler, Peter J.; Messori, Luigi; Metzler-Nolte, Nils | |
| Titolo: | Synthesis and Mode of Action Studies on Iridium(I)–NHC Anticancer Drug Candidates | |
| Anno del prodotto: | 2018 | |
| Abstract: | We report the synthesis, characterization, and biological activity of IrIcomplexes with triazole- (NNHC) and thiazole-based (NSHC) N-heterocyclic carbene ligands. Starting from the dimeric [Ir(COD)Cl]2, we obtained complexes of composition Ir(COD)(NNHC)Cl (4a), Ir(COD)(NNHC)X (4b: X = Cl; 4bBr: X = Br), [Ir(COD)(NNHC)(NHC)]I (5a), [Ir(COD)(NSHC)2]Cl (6a), and [Ir(COD)(NSHC)(NNHC)]Cl (6b) by adaptation of established synthetic methods for metal–NHC complexes. Their interactions with model proteins cytochrome c and lysozyme, as well as with the oligonucleotide hexamer (CG)3(ODN1), were studied. Although most complexes did not show any strong interactions with these biomolecules, all complexes were active against HT-29 and MCF-7 cancerous cells, with IC50values ranging between 1 and 60 µm. The most active compounds were the cationic bis(carbene) derivatives 5 and 6. All compounds generated high levels of reactive oxygen species (ROS) after incubation for 48 h in MCF-7 cells, possibly suggesting a redox-mediated mechanism of action. Interestingly, there were distinctive differences in the superoxide/(total ROS) ratios induced by the different groups of compounds. | |
| Digital Object Identifier (DOI): | 10.1002/ejic.201800225 | |
| Appare nelle tipologie: | 1.1 Articolo in rivista |
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|---|---|---|---|---|
| Synthesis and Mode of Action Studies on Iridium(I)_NHC Anticancer Drug Candidates.pdf | Synthesis and Mode of Action Studies on Iridium(I)_NHC Anticancer Drug Candidates | Versione finale editoriale | NON PUBBLICO - Accesso privato/ristretto | Utenti riconosciuti Richiedi una copia |
http://hdl.handle.net/11568/928835
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