4.7 Article

A cancer specific oxaliplatin-releasing Pt(IV)-prodrug

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DALTON TRANSACTIONS
卷 47, 期 19, 页码 6679-6682

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ROYAL SOC CHEMISTRY
DOI: 10.1039/c8dt01458b

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  1. German Research Council (DFG) [MO 1418/7-1]
  2. Emerging Field Initiative of Friedrich-Alexander-University of Erlangen-Nuremberg [3_Nat_01]
  3. Interdisciplinary Center of Molecular Materials (ICMM)
  4. EU-project RISE-CLATHROPROBES [778245]

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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 mu M 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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