ArticleJournal of medicinal chemistry2021
COUPY Coumarins as Novel Mitochondria-Targeted Photodynamic Therapy Anticancer Agents.
Article in Journal of medicinal chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.
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Who cites it
29 citing papers in PubMed.
- Coumarin and Curcumin-Metal Complexes as Next-Generation Photosensitizers in Cancer Photodynamic Therapy.International journal of molecular sciences · 2026Review
- π-Extended COUPY Fluorophores for Targeted Near-Infrared Fluorescence and Lifetime Imaging in Live Cells.Angewandte Chemie (International ed. in English) · 2026Article
- Coumarin-Based Hybrids: From Linear Photophysical Properties to Multiphoton Excitation Behavior.ACS physical chemistry Au · 2026Article
- A Deep-Red-Absorbing Osmium(II) Complex as a Photosensitizer for Photodynamic Therapy Inducing Immunogenic Cell Death.Angewandte Chemie (International ed. in English) · 2026Article
- Article
- Pyridinium- and bromine-substituted distyryl-BODIPY dyes for mitochondria-targeted photodynamic therapy.Scientific reports · 2026Article
- Key Chemotypes for the Rational Design of Dual AChE/BACE-1 Inhibitors.Current medicinal chemistry · 2026Review
- Potent Inducers of Paraptosis through Electronic Tuning of Hemicyanine Electrophiles.Journal of the American Chemical Society · 2025Article
- On the Photosensitizing Properties of Aloe-Emodin in Photodynamic Therapy: Insights from the Molecular Modeling.The journal of physical chemistry. B · 2025Article
- Exploring the Phototherapeutic Applications of Mitochondria-Targeted COUPY Photocages of Antitumor Drugs.Journal of medicinal chemistry · 2025Article
- Coumarins in Anticancer Therapy: Mechanisms of Action, Potential Applications and Research Perspectives.Pharmaceutics · 2025Review
- Integrative multi-omics data provide insights into the biosynthesis of furanocoumarins and mechanisms regulating their accumulation in Angelica dahurica.Communications biology · 2025Article
- Serendipitous Discovery of Photolytic Thiosulfoxide Formation: Application for Visible-Light-Inducible Manipulation of Supersulfide Level in Biological Systems.Journal of the American Chemical Society · 2025Article
- Plant-derived products as anti-leishmanials which target mitochondria: a review.Expert reviews in molecular medicine · 2025Review
- Ruthenium(II) Polypyridyl Complexes Containing COUBPY Ligands as Potent Photosensitizers for the Efficient Phototherapy of Hypoxic Tumors.Journal of the American Chemical Society · 2025Article
- Modification in Structures of Active Compounds in Anticancer Mitochondria-Targeted Therapy.International journal of molecular sciences · 2025Review
- A Nanoencapsulated Ir(III)-Phthalocyanine Conjugate as a Promising Photodynamic Therapy Anticancer Agent.ACS applied materials & interfaces · 2024Article
- Ir(III) Half-Sandwich Photosensitizers with a π-Expansive Ligand for Efficient Anticancer Photodynamic Therapy.Journal of medicinal chemistry · 2024Article
- Latest developments in coumarin-based anticancer agents: mechanism of action and structure-activity relationship studies.RSC medicinal chemistry · 2024Review
- Small molecules and conjugates as theranostic agents.RSC chemical biology · 2023Review
Corrections and comments
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Authors and funding
7 authors.
Funding
No grant is acknowledged in the PubMed record.
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 hypoxia (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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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.