ArticlePLoS neglected tropical diseases2021
Chalcones identify cTXNPx as a potential antileishmanial drug target.
Article in PLoS neglected tropical diseases, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
15 citing papers in PubMed, 31 citations in OpenAlex.
- Design, synthesis, biological evaluation, and in silico characterization of chalcone derivatives as antidiabetic hits.Scientific reports · 2026Article
- Cross-Species Hepatic Metabolism of the Antileishmanial Chalcone NAT22 Generates Metabolites with Predicted Enhanced Affinity for the Parasite Target cTXNPx.Pharmaceutics · 2026Article
- Chalcones as Multi-target Ligands for Alzheimer's Disease: A Review of Synthetic Strategies and Therapeutic Promise.Mini reviews in medicinal chemistry · 2026Review
- Design of Hybrid Quinoline-Chalcone Compounds AgainstPharmaceuticals (Basel, Switzerland) · 2025Article
- Nanocrystallization Effectively Improves the Oral Efficacy of an Antileishmanial Chalcone.Pharmaceutics · 2025Article
- A Virtual Screening Approach to Evaluate the Multitarget Potential of a Chalcone Library with Binding Properties to Oligopeptidase B and Cysteine Proteinase B fromInternational journal of molecular sciences · 2025Article
- Microwave-Assisted Synthesis of Morpholine-Based Chalcones as Reversible MAO-A Inhibitors in the Management of Mental Depression.Pharmaceuticals (Basel, Switzerland) · 2025Article
- Identification of a New Pentafluorosulfanyl-Substituted Chalcone with Activity Against Hepatoma and Human Parasites.Pharmaceuticals (Basel, Switzerland) · 2025Article
- Applications of CRISPR in Parasitology.Current pharmaceutical biotechnology · 2025Review
- Anti-Pathogens (Basel, Switzerland) · 2024Article
- Chalcone Derivative Induces Flagellar Disruption and Autophagic Phenotype inPathogens (Basel, Switzerland) · 2023Article
- In Vivo Safety and Efficacy of Chalcone-Loaded Microparticles with Modified Polymeric Matrix against Cutaneous Leishmaniasis.Pharmaceutics · 2022Article
- Antileishmanial Activity of 4,8-Dimethoxynaphthalenyl Chalcones onAntibiotics (Basel, Switzerland) · 2022Article
- Review
- Total Synthesis of the Natural Chalcone Lophirone E, Synthetic Studies toward Benzofuran and Indole-Based Analogues, and Investigation of Anti-Leishmanial Activity.Molecules (Basel, Switzerland) · 2022Article
Corrections and comments
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Authors and funding
16 authors at 2 institutions in 2 countries.
Funding
Abstract
With current drug treatments failing due to toxicity, low efficacy and resistance; leishmaniasis is a major global health challenge that desperately needs new validated drug targets. Inspired by activity of the natural chalcone 2',6'-dihydroxy-4'-methoxychalcone (DMC), the nitro-analogue, 3-nitro-2',4',6'- trimethoxychalcone (NAT22, 1c) was identified as potent broad spectrum antileishmanial drug lead. Structural modification provided an alkyne containing chemical probe that labelled a protein within the parasite that was confirmed as cytosolic tryparedoxin peroxidase (cTXNPx). Crucially, labelling is observed in both promastigote and intramacrophage amastigote life forms, with no evidence of host macrophage toxicity. Incubation of the chalcone in the parasite leads to ROS accumulation and parasite death. Deletion of cTXNPx, by CRISPR-Cas9, dramatically impacts upon the parasite phenotype and reduces the antileishmanial activity of the chalcone analogue. Molecular docking studies with a homology model of in-silico cTXNPx suggest that the chalcone is able to bind in the putative active site hindering access to the crucial cysteine residue. Collectively, this work identifies cTXNPx as an important target for antileishmanial chalcones.
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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.