Synthesis and characterization of novel bis(carboxylato) dichloridobis(ethylamine)platinum(IV) complexes with higher cytotoxicity than cisplatin
- Author(s)
- Hristo Varbanov, Seied Mojtaba Valiahdi, Anton Legin, Michael Jakupec, Alexander Roller, Mathea Sophia Galanski, Bernhard Keppler
- Abstract
A series of six novel bis(carboxylato)dichloridobis(ethylamine)platinum(IV) complexes was synthesized and characterized in detail by elemental analysis, FT-IR, ESI-MS, HPLC, multinuclear (1H, 13C, 15N, 195Pt) NMR spectroscopy and in one case by X-ray diffraction. Cytotoxic properties of the complexes were evaluated in four human tumor cell lines originating from ovarian carcinoma (CH1 and SK-OV-3), colon carcinoma (SW480) and non-small cell lung cancer (A549) by means of the MTT colorimetrical assay. In addition, their octanol/water partition coefficients (log P values) were determined. Remarkably the most active (and also most lipophilic) compounds, having 4-propyloxy-4-oxobutanoato and 4-(2-propyloxy)-4-oxobutanoato axial ligands, showed IC50 values down to the low nanomolar range.
- Organisation(s)
- Department of Inorganic Chemistry
- Journal
- European Journal of Medicinal Chemistry
- Volume
- 46
- Pages
- 5456-5464
- No. of pages
- 9
- ISSN
- 0223-5234
- Publication date
- 2011
- Peer reviewed
- Yes
- Austrian Fields of Science 2012
- 104003 Inorganic chemistry, 301305 Medical chemistry
- Sustainable Development Goals
- SDG 3 - Good Health and Well-being
- Portal url
- https://ucrisportal.univie.ac.at/en/publications/2acc398a-2523-478a-817a-696b26d297fe