Fluorescent palladium(II) and platinum(II) NHC/1,2,3-triazole complexes: antiproliferative activity and selectivity against cancer cells
| Autor: | Fritz E. Kühn, Angela Weigert Muñoz, Christian H. G. Jakob, Thomas F. Gronauer, Stephan A. Sieber, Kevin Meighen-Berger, Vanessa Weiß, Jonas F. Schlagintweit, João D. G. Correia, Matthias J. Feige |
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| Rok vydání: | 2021 |
| Předmět: |
Denticity
1 2 3-Triazole Cell Survival chemistry.chemical_element Antineoplastic Agents Medicinal chemistry Fluorescence Cell Line Inorganic Chemistry HeLa chemistry.chemical_compound Coordination Complexes Coumarins Neoplasms Organometallic Compounds Humans Cell Proliferation Platinum biology Chemistry Ligand Triazoles biology.organism_classification Microscopy Fluorescence Selectivity Palladium |
| Zdroj: | Dalton transactions (Cambridge, England : 2003). 50(6) |
| ISSN: | 1477-9234 |
| Popis: | Fluorescent Pd(II) and Pt(II) complexes bearing 4-methylene-7-methoxycoumarin (MMC) and 2,6-diispropylphenyl (Dipp) substituted NHC/1,2,3-triazole hybrid ligands are described. Depending on the reaction conditions two different ligand coordination modes are observed, i.e., bidentate solely coordinating via NHCs or tetradentate coordinating via NHCs and 1,2,3-triazoles. All Dipp substituted complexes show antiproliferative activity against cervix (HeLa) and breast (MCF-7) human carcinoma cells. The activity significantly depends on the coordination mode, with the tetradentate motif being notably more effective (HeLa: IC50 = 3.9 μM to 4.7 μM; MCF-7: IC50 = 2.07 μM to 2.35 μM). Amongst the MMC series, only the Pd(II) complex featuring the bidentate coordination mode is active against HeLa (IC50 = 6.1 μM). In contrast to its structurally related Dipp derivative (SI = 0.6), it shows a high selectivity for HeLa (SI > 16) compared to healthy skin cells (HaCaT). According to fluorescence microscopy, this compound is presumably located in late endosomes or lysosomes. |
| Databáze: | OpenAIRE |
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