A series of 6 substitutionally inert and luminescent iridium(iii) antitumor agents of the type [Ir(C∧N)2(N∧N)][PF6] containing a benzimidazole N∧N ligand with an ester group as a handle for further functionalization has been prepared. They exhibit IC50 values in the high nanomolar range in some ovarian and breast cancer cell lines (approximately 100× more cytotoxic than cisplatin (CDDP) in MDA-MB-231) and are located in the actin cortex predominantly as shown by confocal luminescence microscopy. This discovery could open the door to a new large family of drug bioconjugates with diverse and simultaneous functions.

Departamento de Química Inorgánica and Regional Campus of International Excellence Campus Mare Nostrum Universidad de Murcia and Biomedical Research Institute of Murcia E 30071 Murcia Spain

Institut für Anorganische Chemie und Strukturchemie Heinrich Heine Universität Düsseldorf Universitätsstrasse 1 D 40225 Düsseldorf Germany

Institute of Biophysics Academy of Sciences of the Czech Republic v v i Kralovopolska 135 612 65 Brno Czech Republic

Institute of Biophysics Academy of Sciences of the Czech Republic v v i Kralovopolska 135 612 65 Brno Czech Republic and Department of Biophysics Faculty of Science Palacky University Slechtitelu 27 783 71 Olomouc Czech Republic

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Ir(III) Compounds Containing a Terdentate Ligand Are Potent Inhibitors of Proliferation and Effective Antimetastatic Agents in Aggressive Triple-Negative Breast Cancer Cells