ArticleBiomedicines2021
Target-Oriented Synthesis of Marine Coelenterazine Derivatives with Anticancer Activity by Applying the Heavy-Atom Effect.
Article in Biomedicines, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed, 26 citations in OpenAlex.
- Untargeted Diversity-Oriented Synthesis for the Discovery of New Antitumor Agents: An Integrated Approach of Inverse Virtual Screening, Bioinformatics, and Omics for Target Deconvolution.Journal of medicinal chemistry · 2025Article
- DeepAR: a novel deep learning-based hybrid framework for the interpretable prediction of androgen receptor antagonists.Journal of cheminformatics · 2023Article
- Combined Experimental and Theoretical Investigation into the Photophysical Properties of Halogenated Coelenteramide Analogs.Molecules (Basel, Switzerland) · 2022Article
- Investigation of the Anticancer and Drug Combination Potential of Brominated Coelenteramines toward Breast and Prostate Cancer.International journal of molecular sciences · 2022Article
- Photodynamic Therapy.Biomedicines · 2022Article
- Comparative Investigation of the Chemiluminescent Properties of a Dibrominated Coelenterazine Analog.International journal of molecular sciences · 2022Article
- Discovery of the Anticancer Activity for Lung and Gastric Cancer of a Brominated Coelenteramine Analog.International journal of molecular sciences · 2022Article
- Tuning the Intramolecular Chemiexcitation of Neutral Dioxetanones by Interaction with Ionic Species.Molecules (Basel, Switzerland) · 2022Article
- Theoretical Study of the Thermolysis Reaction and Chemiexcitation of Coelenterazine Dioxetanes.The journal of physical chemistry. A · 2022Article
- Photodynamic therapy for prostate cancer: Recent advances, challenges and opportunities.Frontiers in oncology · 2022Review
- Application of TD-DFT Theory to Studying Porphyrinoid-Based Photosensitizers for Photodynamic Therapy: A Review.Molecules (Basel, Switzerland) · 2021Review
Corrections and comments
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Authors and funding
8 authors at 1 institution in 1 country.
Funding
Abstract
Photodynamic therapy (PDT) is an anticancer therapeutic modality with remarkable advantages over more conventional approaches. However, PDT is greatly limited by its dependence on external light sources. Given this, PDT would benefit from new systems capable of a light-free and intracellular photodynamic effect. Herein, we evaluated the heavy-atom effect as a strategy to provide anticancer activity to derivatives of coelenterazine, a chemiluminescent single-molecule widespread in marine organisms. Our results indicate that the use of the heavy-atom effect allows these molecules to generate readily available triplet states in a chemiluminescent reaction triggered by a cancer marker. Cytotoxicity assays in different cancer cell lines showed a heavy-atom-dependent anticancer activity, which increased in the substituent order of hydroxyl < chlorine < bromine. Furthermore, it was found that the magnitude of this anticancer activity is also dependent on the tumor type, being more relevant toward breast and prostate cancer. The compounds also showed moderate activity toward neuroblastoma, while showing limited activity toward colon cancer. In conclusion, the present results indicate that the application of the heavy-atom effect to marine coelenterazine could be a promising approach for the future development of new and optimized self-activating and tumor-selective sensitizers for light-free PDT.
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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.