Biological Investigations of Ru(II) Complexes with Diverse β-Diketone Ligands

Raphael T. Ryan, Dmytro Havrylyuk, Kimberly C. Stevens, L. Henry Moore, Sean Parkin, Jessica S. Blackburn, David K. Heidary, John P. Selegue, Edith C. Glazer

Research output: Contribution to journalArticlepeer-review

7 Scopus citations


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 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.

Original languageEnglish
Pages (from-to)3611-3621
Number of pages11
JournalEuropean Journal of Inorganic Chemistry
Issue number35
StatePublished - Sep 21 2021

Bibliographical note

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© 2021 Wiley-VCH GmbH.


  • Antitumor agents
  • Cytotoxicity
  • Photophysics
  • Ruthenium

ASJC Scopus subject areas

  • Inorganic Chemistry


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