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A new C,N-cyclometalated osmium(ii) arene anticancer scaffold with a handle for functionalization and antioxidative
Enrique Ortega1, Jyoti G Yellol, Matthias Rothemund
1Departamento de Química Inorgánica and Regional Campus of International Excellence "Campus Mare Nostrum", Universidad de Murcia, and Biomedical Research Institute of Murcia (IMIB-Arrixaca), E-30071 Murcia, Spain. jruiz@um.es.
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.
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