2021 journal article
Biological Investigations of Ru(II) Complexes with Diverse β‐Diketone Ligands
European Journal of Inorganic Chemistry, 2021(35), 3611–3621.
author keywords: Antitumor agents; Cytotoxicity; Photophysics; Ruthenium
TL;DR:
It is suggested 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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Added: January 29, 2023
AbstractThe β‐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.