In:
European Journal of Inorganic Chemistry, Wiley, Vol. 2021, No. 35 ( 2021-09-21), p. 3611-3621
Abstract:
The 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 κ 2 ‐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 κ 2 ‐O,O’‐ligands can be incorporated into Ru(II)‐polypyridyl complexes to create favorable candidates for future drug development.
Type of Medium:
Online Resource
ISSN:
1434-1948
,
1099-0682
DOI:
10.1002/ejic.v2021.35
DOI:
10.1002/ejic.202100468
Language:
English
Publisher:
Wiley
Publication Date:
2021
detail.hit.zdb_id:
1475009-0
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