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Issue 24, 2015
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Design, synthesis and characterisation of new chimeric ruthenium(II)–gold(I) complexes as improved cytotoxic agents

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Abstract

Two heterobimetallic complexes, i.e. [RuCl2(p-cymene)(μ-dppm)AuC] (1) and [RuCl2(p-cymene)(μ-dppm)Au(S-thiazoline)] (3), based on known cytotoxic [Ru(p-cymene)Cl2(PR3)] and [AuX(PR3)] (X = Cl, SR) molecular scaffolds, with the diphosphane linker 1,1-bis(diphenylphosphino)methane, dppm, were conveniently prepared and characterised. Remarkably, the new compounds manifested a more favourable in vitro pharmacological profile toward cancer cells than individual ruthenium and gold species being either more cytotoxic or more selective. The interactions of the studied compounds with (pBR322) DNA and their inhibitory effects on cathepsin B were also assessed. In addition, their reactivity toward suitable models of protein targets was explored and clear evidence gained for disruption of the bimetallic motif and for protein binding of monometallic fragments. Overall, the data reported here strongly support the concept of multifunctional heterometallic compounds as “improved” candidate agents for cancer treatment. The mechanistic and pharmacological implications of the present findings are discussed.

Graphical abstract: Design, synthesis and characterisation of new chimeric ruthenium(ii)–gold(i) complexes as improved cytotoxic agents

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Publication details

The article was received on 25 Mar 2015, accepted on 05 May 2015 and first published on 05 May 2015


Article type: Paper
DOI: 10.1039/C5DT01614B
Author version available: Download Author version (PDF)
Citation: Dalton Trans., 2015,44, 11067-11076
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    Design, synthesis and characterisation of new chimeric ruthenium(II)–gold(I) complexes as improved cytotoxic agents

    L. Massai, J. Fernández-Gallardo, A. Guerri, A. Arcangeli, S. Pillozzi, M. Contel and L. Messori, Dalton Trans., 2015, 44, 11067
    DOI: 10.1039/C5DT01614B

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