Carregant...
Fitxers
Tipus de document
ArticleVersió
Versió publicadaData de publicació
Llicència de publicació
Si us plau utilitzeu sempre aquest identificador per citar o enllaçar aquest document: https://hdl.handle.net/2445/183273
COUPY Coumarins as Novel Mitochondria-Targeted Photodynamic Therapy Anticancer Agents
Títol de la revista
Director/Tutor
ISSN de la revista
Títol del volum
Recurs relacionat
Resum
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.
Matèries
Matèries (anglès)
Citació
Citació
ORTEGA FORTE, Enrique, ROVIRA, Anna, GANDIOSO, Albert, BONELLI BLASCO, Joaquin daniel, BOSCH MARIMON, Manel, RUIZ, José, MARCHÁN SANCHO, Vicente. COUPY Coumarins as Novel Mitochondria-Targeted Photodynamic Therapy Anticancer Agents. _Journal of Medicinal Chemistry_. 2021. Vol. 64, núm. 23, pàgs. 17209-17220. [consulta: 30 de gener de 2026]. ISSN: 0022-2623. [Disponible a: https://hdl.handle.net/2445/183273]