Biological Investigations of Ru(II) Complexes With Diverse ß-diketone Ligands.
Eur J Inorg Chem
; 2021(35): 3611-3621, 2021 Sep 21.
Article
em En
| MEDLINE
| ID: mdl-34539235
ABSTRACT
The ß-diketone scaffold is a commonly used synthetic intermediate, and is a functional group found in natural products such as curcuminoids. This core structure can also act as a chelating ligand for a variety of metals. In order to assess the potential of this scaffold for medicinal inorganic chemistry, seven different κ2-O,O'-chelating ligands were used to construct Ru(II) complexes with polypyridyl co-ligands, and their biological activity was evaluated. The complexes demonstrated promising structure-dependent cytotoxicity. Three complexes maintained high activity in a tumor spheroid model, and all complexes demonstrated low in vivo toxicity in a zebrafish model. From this series, the best compound exhibited a ~ 30-fold window between cytotoxicity in a 3-D tumor spheroid model and potential in vivo toxicity. These results suggest that κ2-O,O'-ligands can be incorporated into Ru(II)-polypyridyl complexes to create favorable candidates for future drug development.
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Base de dados:
MEDLINE
Idioma:
En
Revista:
Eur J Inorg Chem
Ano de publicação:
2021
Tipo de documento:
Article
País de afiliação:
Estados Unidos