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Graf, Marion; Gothe, Yvonne; Siegmund, Daniel; Metzler-Nolte, Nils; Suenkel, Karlheinz (2018): Synthesis and characterization of cyclometallated rhodium(III) and iridium(III) compounds with antiproliferative activities in the nanomolar range. In: Inorganica Chimica Acta, Vol. 471: pp. 265-271
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Abstract

The reaction of the dimeric cyclometalated complexes [{M(mu-Cl)(ptpy)(2)}(2)] with symmetrical di alkyl-substituted bipyridines followed by metathesis with KPF6 yields the complex salts [M(ptpy)(2)(6,6'-dimethyl-bipyridine)]PF6 and [M(ptpy)(2)(4,4'-dialkyl-bipyridine)]PF6, (M = Rh, Ir;alkyl = methyl, n-Propyl, t-Butyl or n-nonyl, ptpy = 2-(p-tolyl)pyridinato). All compounds were characterized by elemental analyses, mass spectra and H-1 and C-13 NMR spectra. The compounds 1, 6, 7, 8, 10 were also examined by X-ray crystallography and their proposed octahedral tris-chelate structure with trans configuration of the cyclometalating tolylpyridinato N atoms was proven. All compounds display significant cytotoxicity against human cancer cell lines MCF-7 and HT-29. The most active compounds in this study display IC50 values down to 120 nM, making them two orders of magnitude more active than the established anticancer drug cisplatin.