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Towards Novel Photodynamic Anticancer Agents Generating Superoxide Anion Radicals: A Cyclometalated Ir III Complex Conjugated to a Far‐Red Emitting Coumarin
Author(s) -
Novohradsky Vojtech,
Rovira Anna,
Hally Cormac,
Galindo Alex,
Vigueras Gloria,
Gandioso Albert,
Svitelova Marie,
BresolíObach Roger,
Kostrhunova Hana,
Markova Lenka,
Kasparkova Jana,
ll Santi,
Ruiz José,
Brabec Viktor,
Marchán Vicente
Publication year - 2019
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201901268
Subject(s) - photodynamic therapy , superoxide , chemistry , reactive oxygen species , hela , photochemistry , radical , conjugated system , coumarin , cytotoxicity , fluorescence , far red , cancer cell , combinatorial chemistry , cancer , biochemistry , organic chemistry , cell , red light , in vitro , medicine , biology , physics , quantum mechanics , enzyme , polymer , botany
Although cyclometalated Ir III 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 Ir III complex conjugated to a far‐red‐emitting coumarin, Ir III –COUPY, is reported with highly favourable properties for cancer phototherapy. Ir III –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.

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