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Exploring Structure-Activity Relationships in Photodynamic Therapy Anticancer Agents Based on Ir(III)-COUPY

Anna Rovira1, Enrique Ortega-Forte2, Cormac Hally3

  • 1Departament de Química Inorgànica i Orgànica, Secció de Química Orgànica, Universitat de Barcelona (UB), and Institut de Biomedicina de la Universitat de Barcelona (IBUB), Martí i Franquès 1-11, E-08028 Barcelona, Spain.

Journal of Medicinal Chemistry
|June 2, 2023
PubMed

Insights

Researchers developed novel photodynamic therapy (PDT) agents using iridium(III)-COUPY conjugates to combat drug-resistant cancers. These agents show high phototoxicity and effectiveness even in hypoxic conditions, offering a promising non-invasive treatment for cisplatin-resistant cells.

Area of Science:

  • Chemistry
  • Biomedical Engineering
  • Oncology

Background:

  • Photodynamic therapy (PDT) is a promising non-invasive treatment for drug-resistant cancers.
  • Development of effective, non-toxic photosensitizers, especially for hypoxic conditions, is crucial.

Purpose of the Study:

  • To design and synthesize novel PDT agents based on iridium(III)-COUPY conjugates.
  • To explore structure-activity relationships influencing photophysical properties and anticancer efficacy.
  • To evaluate the efficacy of these agents against cisplatin-resistant cancer cells under normoxic and hypoxic conditions.

Main Methods:

  • Synthesis of iridium(III)-COUPY conjugates with structural modifications on the coumarin scaffold.
  • Characterization of photophysical properties (e.g., phototoxicity, ROS generation).
  • In vitro evaluation of cellular uptake and phototherapeutic efficacy in A2780cis cancer cells.

Main Results:

  • Structural modifications of the coumarin scaffold significantly impacted photophysical properties and cellular uptake.
  • All synthesized Ir(III)-COUPY conjugates demonstrated high phototoxicity under green light irradiation via reactive oxygen species (ROS) generation.
  • Two lead conjugates exhibited significant phototherapeutic effects in cisplatin-resistant A2780cis cells, even under hypoxic conditions.

Conclusions:

  • Ir(III)-COUPY conjugates are effective PDT agents with potent anticancer activity.
  • These agents can overcome acquired cisplatin resistance in cancer cells.
  • Conjugation of far-red/NIR-emitting COUPY dyes with transition metal complexes offers a viable strategy for advanced phototherapy.

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