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A cancer specific oxaliplatin-releasing Pt(iv)-prodrug
Viktor Reshetnikov1, Anton Arkhypov, Purushottam Reddy Julakanti
1Friedrich-Alexander-University of Erlangen-Nürnberg, Department of Chemistry and Pharmacy, Organic Chemistry Chair II, Nikolaus-Fiebiger-Str. 10, 91058 Erlangen, Germany. Andriy.Mokhir@fau.de.
Abstract:
We prepared a Pt(iv)-prodrug, which under cancer specific conditions (elevated concentration of reactive oxygen species, ROS) releases a DNA-binding drug oxaliplatin as well as ROS-amplifying drugs p-quinone methide and N-alkylferrocenium. Due to the concerted action of these components, an excellent anticancer effect was achieved: IC50 = 0.4 ± 0.1 μM for human ovarian carcinoma A2780 cells. Importantly, the prodrug was found to be 45-fold less toxic to normal cells (HDFa).
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