Towards Novel Photodynamic Anticancer Agents Generating Superoxide Anion Radicals: A Cyclometalated IrIII Complex Conjugated to a Far-Red Emitting Coumarin

Vojtech Novohradsky, Anna Rovira, Cormac Hally, Alex Galindo, Gloria Vigueras, Albert Gandioso, Marie Svitelova, Roger Bresolí-Obach, Hana Kostrhunova, Lenka Markova, Jana Kasparkova, Santi Nonell, José Ruiz, Viktor Brabec, Vicente Marchán

Research output: Indexed journal article Articlepeer-review

136 Citations (Scopus)

Abstract

Although cyclometalated IrIII complexes have emerged as promising photosensitizers for photodynamic therapy, some key drawbacks still hamper clinical translation, such as operability in the phototherapeutic window and reactive oxygen species (ROS) production efficiency and selectivity. In this work, a cyclometalated IrIII complex conjugated to a far-red-emitting coumarin, IrIII–COUPY, is reported with highly favourable properties for cancer phototherapy. IrIII–COUPY was efficiently taken up by HeLa cells and showed no dark cytotoxicity and impressive photocytotoxicity indexes after irradiation with green and blue light, even under hypoxia. Importantly, a clear correlation between cell death and intracellular generation of superoxide anion radicals after visible light irradiation was demonstrated. This strategy opens the door to novel fluorescent photodynamic therapy agents with promising applications in theragnosis.

Original languageEnglish
Pages (from-to)6311-6315
Number of pages5
JournalAngewandte Chemie - International Edition
Volume58
Issue number19
DOIs
Publication statusPublished - 6 May 2019

Keywords

  • conjugation
  • coumarin
  • cyclometalated iridium(III) complexes
  • photodynamic therapy
  • photosensitizer

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