Synthesis, characterization, and in vitro cytotoxicity of a Kiteplatin-Ibuprofen Pt(IV) prodrug

Alessandra Curci, Nunzio Denora, Rosa Maria Iacobazzi, Nicoletta Ditaranto, James D. Hoeschele, Nicola Margiotta, Giovanni Natile

Research output: Contribution to journalArticlepeer-review


The Pt(IV) prodrug of kiteplatin, cis-trans-cis-[PtCl2(RS-Ibuprofen-H)2(cis-1,4-DACH)], having in the axial positions two molecules of Ibuprofen, has been synthesised, characterized and tested in vitro. The aim was to potentiate the cytotoxic effect of kiteplatin with the anti-inflammatory activity of Ibuprofen. The reduction potential of the conjugate resulted comparable to those of other reported Pt(IV) carboxylate complexes, ensuring in vivo stability in blood during transport and intracellular reduction with release of the active species. The cytotoxic activity of the complex resulted remarkably potentiated reaching nanomolar activity. It is possible that the coordinated Ibuprofen molecules promote the transport and the accumulation of the complex in tumor cells by increasing its lipophilicity. In addition to the increased uptake, Ibuprofen could also exert an anti-inflammatory action mediated by inhibition of the COX enzymes which are overexpressed in tumors. The use of a conjugate with Pt-bound Ibuprofen can ensure similar cellular uptake and biodistribution for both the anti-inflammatory and the cytotoxic drugs in the exact ratio of 2:1.

Original languageEnglish
Pages (from-to)221-228
Number of pages8
JournalInorganica Chimica Acta
Publication statusPublished - Mar 1 2018


  • cis-1, 4-DACH
  • Cisplatin
  • Colon cancer
  • Ibuprofen
  • Kiteplatin
  • Pt(IV) drugs

ASJC Scopus subject areas

  • Physical and Theoretical Chemistry
  • Inorganic Chemistry
  • Materials Chemistry


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