ArticlePhotochemistry and photobiology2020
Psoralen Derivatives with Enhanced Potency.
Article in Photochemistry and photobiology, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 38 citations in OpenAlex.
- Pharmacological Mechanisms of Active Constituents from Traditional Chinese Medicine for Vitiligo Treatment.Pharmaceuticals (Basel, Switzerland) · 2026Review
- Development and functional evaluation of a psoralen-conjugated nucleoside mimic for triplex-forming oligonucleotides.Communications chemistry · 2025Article
- From Plant to Patient: A Historical Perspective and Review of Selected Medicinal Plants in Dermatology.JID innovations : skin science from molecules to population health · 2025Review
- Pharmaceutical Design and Structure-activity Relationships of Psoralen and Derivatives.Current pharmaceutical design · 2025Review
- Thio and Seleno Derivatives of Angelicin as Efficient Triplet Harvesting Photosensitizers: Implications in Photodynamic Therapy.Chemphyschem : a European journal of chemical physics and physical chemistry · 2024Article
- DNA-Intercalating Supramolecular Hydrogels for Tunable Thermal and Viscoelastic Properties.Angewandte Chemie (International ed. in English) · 2024Article
- Recent Advancements in Development and Therapeutic Applications of Genome-Targeting Triplex-Forming Oligonucleotides and Peptide Nucleic Acids.Pharmaceutics · 2023Review
- Psoralea corylifolia L.: a comprehensive review of its botany, traditional uses, phytochemistry, pharmacology, toxicology, quality control and pharmacokinetics.Chinese medicine · 2023Review
- Psoralen as a Photosensitizers for Photodynamic Therapy by Means of In Vitro Cherenkov Light.International journal of molecular sciences · 2022Article
- Investigation of cytotoxic and antioxidative activity of 1,2,3-triazolyl-modified furocoumarins and 2,3-dihydrofurocoumarins.Protoplasma · 2022Article
- Anti-Inflammatory Effects of Psoralen Derivatives on RAW264.7 Cells via Regulation of the NF-κB and MAPK Signaling Pathways.International journal of molecular sciences · 2022Article
- Tracing the Photoaddition of Pharmaceutical Psoralens to DNA.Molecules (Basel, Switzerland) · 2020Article
Corrections and comments
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Authors and funding
9 authors at 6 institutions in 1 country.
Funding
Abstract
Psoralen is a furocoumarin natural product that intercalates within DNA and forms covalent adducts when activated by ultraviolet radiation. It is well known that this property contributes to psoralen's clinical efficacy in several disease contexts, which include vitiligo, psoriasis, graft-versus-host disease and cutaneous T-cell lymphoma. Given the therapeutic relevance of psoralen and its derivatives, we attempted to synthesize psoralens with even greater potency. In this study, we report a library of 73 novel psoralens, the largest collection of its kind. When screened for the ability to reduce cell proliferation, we identified two derivatives even more cytotoxic than 4'-aminomethyl-4,5',8-trimethylpsoralen (AMT), one of the most potent psoralens identified to date. Using MALDI-TOF MS, we studied the DNA adduct formation for a subset of novel psoralens and found that in most cases enhanced DNA binding correlated well with cytotoxicity. Generally, our most potent derivatives contain positively charged substituents, which we believe increase DNA affinity and enhance psoralen intercalation. Thus, we provide a rational approach to guide efforts toward further optimizing psoralens to fully capitalize on this drug class' therapeutic potential. Finally, the structure-activity insights we have gained shed light on several opportunities to study currently underappreciated aspects of psoralen's mechanism.
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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.