Cytotoxic Activities of Bis-cyclometalated M(III) Complexes (M=Rh, Ir) Containing 5-substituted 1,10-Phenanthroline or 4,4'-substituted 2,2'-Bipyridine Ligands

Graf, Marion; Böttcher, Hans-Christian; Metzler-Nolte, Nils; Thavalingam, Sugina und Mayer, Peter (2022): Cytotoxic Activities of Bis-cyclometalated M(III) Complexes (M=Rh, Ir) Containing 5-substituted 1,10-Phenanthroline or 4,4'-substituted 2,2'-Bipyridine Ligands. In: Zeitschrift für Anorganische und Allgemeine Chemie, Bd. 648, Nr. 21

Abstract

The synthesis and characterization of eight new bis-cyclometalated compounds [M(ptpy)(2)(N<^>N)]PF6 (ptpy=2-(p-tolyl)pyridinato;N<^>N=5-chloro-1,10-phenanthroline: M=Rh, 1;M=Ir, 2);N<^>N=5-methyl-1,10-phenanthroline: M=Rh, 3;M=Ir, 4;N<^>N=4,4'-diphenyl-2,2'-bipyridine: M=Rh, 5;M=Ir, 6;N<^>N=4,4'-diamino-2,2'-bipyridine: M=Rh, 7;M=Ir, 8) are described. All compounds were characterized by spectroscopic means. Additionally, the molecular structures of compounds 4, 5, 6, and 8 in the crystal were determined by single-crystal X-ray diffraction studies. To explore the cytotoxic properties of all new eight compounds, colorimetric assays (MTT assay) against prominent cancer cell lines, MCF-7 and HT-29, were performed. The determined IC50 values are in the low micromolar range, between 1.3-5.6 mu M. The most effective compounds are 1 and 2 with 5-chloro-substituted phenanthroline ligands, whereas the diamino-substituted bipyridine ligands (5 and 6) are the least cytotoxic compounds. The tested complexes showed a significant increase in cytotoxicity, up to 25-fold increase in MCF-7 cancer cells, and up to 60-fold increase in the HT-29 cell line compared to the established anticancer compound cisplatin under identical conditions.

• Dokumententyp: Zeitschriftenartikel
• Fakultät: Chemie und Pharmazie > Department Chemie
• Themengebiete: 500 Naturwissenschaften und Mathematik > 540 Chemie
• ISSN: 0044-2313
• Sprache: Englisch
• DFG: Gefördert durch die Deutsche Forschungsgemeinschaft (DFG) - 491502892