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Issue 3, 2014
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Ruthenium(II) and osmium(II) 1,2,3-triazolylidene organometallics: a preliminary investigation into the biological activity of ‘click’ carbene complexes

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Abstract

Taking advantage of the facile and versatile synthetic properties of ‘click’ 1,2,3-triazolylidene N-heterocyclic carbenes (tzNHC's), a range of new organometallic Ru(II) and Os(II) arene complexes containing functionalised tzNHC ligands, [M(η6-p-cymene)(tzNHC)Cl2] [M = Ru(II), Os(II)], have been synthesised and fully characterised, including the X-ray crystal structure of one of the Os(II) complexes. The tzNHC ligands remain coordinated to the metal centres under relevant physiological conditions, and following binding to the model protein, ubiquitin. The in vitro cytotoxicity of the compounds towards human ovarian cancer cells is dependent on the substituent on the tzNHC ligand but is generally <50 μM and in some cases <1 μM, whilst still retaining a high degree of selectivity towards cancer cells over healthy cells (1.85 μM in A2780 ovarian cancer cells versus 435 μM in human embryonic kidney cells in one case).

Graphical abstract: Ruthenium(ii) and osmium(ii) 1,2,3-triazolylidene organometallics: a preliminary investigation into the biological activity of ‘click’ carbene complexes

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Publication details

The article was received on 18 Sep 2013, accepted on 30 Oct 2013 and first published on 30 Oct 2013


Article type: Paper
DOI: 10.1039/C3DT52584H
Citation: Dalton Trans., 2014,43, 1443-1448
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    Ruthenium(II) and osmium(II) 1,2,3-triazolylidene organometallics: a preliminary investigation into the biological activity of ‘click’ carbene complexes

    K. J. Kilpin, S. Crot, T. Riedel, J. A. Kitchen and P. J. Dyson, Dalton Trans., 2014, 43, 1443
    DOI: 10.1039/C3DT52584H

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