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Title: COUPY Coumarins as Novel Mitochondria-Targeted Photodynamic Therapy Anticancer Agents
Author: Ortega-Forte, Enrique
Rovira, Anna
Gandioso, Albert
Bonelli, Joaquín
Bosch Marimon, Manel
Ruiz, José
Marchán Sancho, Vicente
Keywords: Cumarines
Medicaments antineoplàstics
Antineoplastic agents
Issue Date: 19-Nov-2021
Publisher: American Chemical Society
Abstract: Photodynamic therapy (PDT) for cancer treatment has drawn increased attention over the last decades. Herein, we introduce a novel family of low-molecular-weight coumarins as potential PDT anticancer tools. Through a systematic study with a library of 15 compounds, we have established a detailed structure−activity relationship rationale, which allowed the selection of three lead compounds exhibiting effective in vitro anticancer activities upon visible-light irradiation in both normoxia and hipoxia (phototherapeutic indexes up to 71) and minimal toxicity toward normal cells. Acting as excellent theranostic agents targeting mitochondria, the mechanism of action of the photosensitizers has been investigated in detail in HeLa cells. The generation of cytotoxic reactive oxygen species, which has been found to be a major contributor of the coumarins' phototoxicity, and the induction of apoptosis and/or autophagy have been identified as the cell death modes triggered after irradiation with low doses of visible light.
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It is part of: Journal of Medicinal Chemistry, 2021, vol. 64, num. 23, p. 17209-17220
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ISSN: 0022-2623
Appears in Collections:Articles publicats en revistes (Química Inorgànica i Orgànica)

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