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Issue 79, 2018
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A new C,N-cyclometalated osmium(ii) arene anticancer scaffold with a handle for functionalization and antioxidative properties

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Abstract

A series of six osmium(II) complexes of the type [(η6-p-cymene)Os(C^N)X] (X = chlorido or acetato) containing benzimidazole C^N ligands with an ester group as a handle for further functionalization have been synthesized. They exhibit IC50 values in the low micromolar range in a panel of cisplatin (CDDP)-resistant cancer cells (approximately 10× more cytotoxic than CDDP in MCF-7), decrease the levels of intracellular ROS and reduce the NAD+ coenzyme, and inhibit tubulin polymerization. This discovery could open the door to a new large family of osmium(II)-based bioconjugates with diverse modes of action.

Graphical abstract: A new C,N-cyclometalated osmium(ii) arene anticancer scaffold with a handle for functionalization and antioxidative properties

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Supplementary files

Article information


Submitted
07 Aug 2018
Accepted
04 Sep 2018
First published
04 Sep 2018

Chem. Commun., 2018,54, 11120-11123
Article type
Communication

A new C,N-cyclometalated osmium(II) arene anticancer scaffold with a handle for functionalization and antioxidative properties

E. Ortega, J. G. Yellol, M. Rothemund, F. J. Ballester, V. Rodríguez, G. Yellol, C. Janiak, R. Schobert and J. Ruiz, Chem. Commun., 2018, 54, 11120
DOI: 10.1039/C8CC06427J

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