Ruthenium(II) complexes of thiosemicarbazones: The first water-soluble complex with pH-dependent antiproliferative activity
- Author(s)
- Vladimir Arion, Bernhard Keppler, Sanja Grguric-Sipka, Christian Kowol, Seied Mojtaba Valiahdi, Rene Eichinger, Michael Jakupec, Alexander Roller, Sergiu Shova
- Abstract
Two ruthenium(II) complexes of 2-acetylpyridine N4,N 4-dimethylthiosemicarbazone (HL1) and phenanthrenequinone thiosemicarbazone (HL2), namely [RuIICl(L 1)(PPh3)2] (1) and [RuIICl(L 2)(PPh3)2] (2), have been synthesised and characterised by IR, UV/Vis and NMR spectroscopy, electrospray mass spectrometry, cyclic voltammetry and X-ray crystallography. In addition, the X-ray crystal structure of [RuIIICl2(L2)- PPh3]·dmso·1.25H2O (3·dmso·1. 25H2O) is reported. The reaction of [RuIICl 2(dmso)4] with HL1 and 1,3,5-triaza-7- phosphaadamantane (PTA) gives the highly water-soluble complex [Ru IICl(L1)(HPTA)2]Cl2·C 2H5OH·H2O (4·C2H 5OH·H2O) (S25°C ? 250 mg/mL), which has been fully characterised. Complex 4 shows strong antiproliferative effects in low micromolar concentrations in the ovarian carcinoma cell line 41M (IC50 = 0.87 ?M) and more moderate activity in the breast cancer cell line SK-BR-3 (IC50 = 39 ?M). The activity of the compound is 6.5- and 5.4-times higher at pH = 6.0 than at pH = 7.4 in the non-small cell lung cancer cell line A549 and the colon carcinoma cell line HT-29 (GI 50 = 24 and 8.0 ?M at pH = 6.0 for A549 and HT-29, respectively). © Wiley-VCH Verlag GmbH & Co. KGaA, 2007.
- Organisation(s)
- Department of Inorganic Chemistry
- Journal
- European Journal of Inorganic Chemistry
- Volume
- 2007
- Pages
- 2870-2878
- No. of pages
- 9
- ISSN
- 1434-1948
- Publication date
- 2007
- Peer reviewed
- Yes
- Austrian Fields of Science 2012
- 104003 Inorganic chemistry
- Sustainable Development Goals
- SDG 3 - Good Health and Well-being
- Portal url
- https://ucrisportal.univie.ac.at/en/publications/f29ed6e8-8f8b-4462-9d8a-556c289d3c9e