Synthesis, crystal structure and pH dependent cytotoxicity of (SP-4-2)-bis(2-aminoethanolato-kappa2N,O)platinum(II) - A representative of novel pH sensitive anticancer platinum complexes
- Author(s)
- Mathea Sophia Galanski, Christian Baumgartner, Kristof Meelich, Vladimir Arion, Madeleine Fremuth, Michael Jakupec, Petra Schluga, Christian Hartinger, Nikolai Graf v. Keyserlingk, Bernhard Keppler
- Abstract
Solid tumors are often hypoxic and consequently the pH in the tumoral tissue is decreasing with increasing tumor size (pH 5.5-7.4 in solid tumors versus pH 7.4 in normal tissues). This marked difference in pH value is a problem for weak base organic drugs and could advantageously be used for the introduction of pH sensitive anticancer platinum drugs. Synthesis and structure determination of (SP-4-2)-bis(2-aminoethanolato-?2N,O) platinum(II), its binding behavior to 5'-GMP and its cytotoxicity against cisplatin sensitive cell lines under standard pH screening conditions (pH 7.4) as well as in acidified cell culture medium (pH 6.0) mimicking the conditions in a number of solid tumors is presented. There is evidence that this concept in anticancer platinum therapy, namely administration of rather unreactive drugs and activation under acidic pH conditions, can be realized. Π2004 Elsevier B.V. All rights reserved.
- Organisation(s)
- Department of Inorganic Chemistry
- External organisation(s)
- Faustus Forschungs Compagnie GmbH
- Journal
- Inorganica Chimica Acta
- Volume
- 357
- Pages
- 3237-3244
- No. of pages
- 8
- ISSN
- 0020-1693
- Publication date
- 2004
- Peer reviewed
- Yes
- Austrian Fields of Science 2012
- 104003 Inorganic chemistry
- Portal url
- https://ucrisportal.univie.ac.at/en/publications/88f2a9e0-255e-4979-85b8-43473b523749