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

Autor: Ortega E; Departamento 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., Yellol JG, Rothemund M, Ballester FJ, Rodríguez V, Yellol G, Janiak C, Schobert R, Ruiz J
Jazyk: angličtina
Zdroj: Chemical communications (Cambridge, England) [Chem Commun (Camb)] 2018 Oct 02; Vol. 54 (79), pp. 11120-11123.
DOI: 10.1039/c8cc06427j
Abstrakt: 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.
Databáze: MEDLINE