Unsymmetric mono- and dinuclear platinum(IV) complexes featuring an ethylene glycol moiety: Synthesis, characterization, and biological activity
- Author(s)
- Verena Pichler, Petra Heffeter, Seied Mojtaba Valiahdi, Christian Kowol, Alexander Egger, Walter Berger, Michael Jakupec, Mathea Sophia Galanski, Bernhard Keppler
- Abstract
Eight novel mononuclear and two dinuclear platinum(IV) complexes were synthesized and characterized by elemental analysis, one- and two-dimensional NMR spectroscopy, mass spectrometry, and reversed-phase HPLC (log kw) and in one case by X-ray diffraction. Cytotoxicity of the compounds was studied in three human cancer cell lines (CH1, SW480, and A549) by means of the MTT assay, featuring IC50 values to the low micromolar range. Furthermore a selected set of compounds was investigated in additional cancer cell lines (P31 and P31/cis, A2780 and A2780/cis, SW1573, 2R120, and 2R160) with regard to their resistance patterns, offering a distinctly different scheme compared to cisplatin. To gain further insights into the mode of action, drug uptake, DNA synthesis inhibition, cell cycle effects, and induction of apoptosis were determined for two characteristic substances.
- Organisation(s)
- Department of Inorganic Chemistry
- External organisation(s)
- Medizinische Universität Wien
- Journal
- Journal of Medicinal Chemistry
- Volume
- 55
- Pages
- 11052-11061
- No. of pages
- 10
- ISSN
- 0022-2623
- DOI
- https://doi.org/10.1021/jm301645g
- Publication date
- 2012
- 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/b248a731-912e-4396-a042-e5610a684429