Synthesis, cytotoxicity, and structure-activity relationships of new oxaliplatin derivatives

Author(s)
Mathea Sophia Galanski, Afshin Yasemi, Michael Jakupec, Nikolai Graf v. Keyserlingk, Bernhard Keppler
Abstract

In order to setup structure-activity relationships and to explore the possibilities of improving the anticancer activity of oxaliplatin, which was recently approved for combination chemotherapy of metastatic colorectal cancer, new oxaliplatin analogues have been synthesized. The cytotoxicity was determined in nine human tumor cell lines and revealed a comparable or even higher cytotoxic potency in leukemia, ovarian and colon cancer cell lines in the case of small substituents at position 4 of the cyclohexane-1,2-diamine ligand. Introduction of bigger substituents at this position and thereby increasing the steric demand of the diamine ligands and the lipophilicity of the oxaliplatin derivatives resulted in platinum complexes with reduced cytotoxic properties. Œ Springer-Verlag 2005.

Organisation(s)
Department of Inorganic Chemistry
External organisation(s)
Faustus Forschungs Compagnie GmbH
Journal
Monatshefte für Chemie
Volume
136
Pages
693-700
No. of pages
8
ISSN
0026-9247
Publication date
2005
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/3a1af1d8-2a8d-4f26-a6a6-40800028a050