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

Mathea Sophia Galanski (Corresponding author), Afshin Yasemi, Michael Jakupec, Nikolai Graf v. Keyserlingk, Bernhard Keppler

Publications: Contribution to journalArticlePeer Reviewed

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.
Original languageEnglish
Pages (from-to)693-700
Number of pages8
JournalMonatshefte für Chemie
Volume136
Issue number5
Publication statusPublished - 2005

Austrian Fields of Science 2012

  • 104003 Inorganic chemistry

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