ArticleJournal of medicinal chemistry2011
Investigating the antimalarial action of 1,2,4-trioxolanes with fluorescent chemical probes.
Article in Journal of medicinal chemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
What it found
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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
16 citing papers in PubMed, 40 citations in OpenAlex.
- Fast autoxidation of unsaturated lipid films on indoor surfaces.Nature communications · 2025Article
- Chemo-proteomics in antimalarial target identification and engagement.Medicinal research reviews · 2023Review
- Peroxide Antimalarial Drugs Target Redox Homeostasis inACS infectious diseases · 2022Article
- Intrinsic fluorescence properties of antimalarial pyrido[1,2-Organic & biomolecular chemistry · 2020Article
- System-wide biochemical analysis reveals ozonide antimalarials initially act by disrupting Plasmodium falciparum haemoglobin digestion.PLoS pathogens · 2020Article
- Virtual design of novel Plasmodium falciparum cysteine protease falcipain-2 hybrid lactone-chalcone and isatin-chalcone inhibitors probing the S2 active site pocket.Journal of enzyme inhibition and medicinal chemistry · 2019Article
- In vitro activity of anti-malarial ozonides against an artemisinin-resistant isolate.Malaria journal · 2017Article
- Monoclonal Antibodies That Recognize the Alkylation Signature of Antimalarial Ozonides OZ277 (Arterolane) and OZ439 (Artefenomel).ACS infectious diseases · 2016Article
- Trioxolane-Mediated Delivery of Mefloquine Limits Brain Exposure in a Mouse Model of Malaria.ACS medicinal chemistry letters · 2015Article
- Drug delivery to the malaria parasite using an arterolane-like scaffold.ChemMedChem · 2015Article
- Synthesis of five- and six-membered cyclic organic peroxides: Key transformations into peroxide ring-retaining products.Beilstein journal of organic chemistry · 2014Review
- Antimalarial activity of 4-metoxychalcones: docking studies as falcipain/plasmepsin inhibitors, ADMET and lipophilic efficiency analysis to identify a putative oral lead candidate.Molecules (Basel, Switzerland) · 2013Article
- Ferrous iron-dependent drug delivery enables controlled and selective release of therapeutic agents in vivo.Proceedings of the National Academy of Sciences of the United States of America · 2013Article
- Hemozoin and antimalarial drug discovery.Future medicinal chemistry · 2013Review
- The lipophilic bullet hits the targets: medicinal chemistry of adamantane derivatives.Chemical reviews · 2013Review
- Ferrous iron-dependent delivery of therapeutic agents to the malaria parasite.Future medicinal chemistry · 2012Article
Corrections and comments
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Authors and funding
6 authors at 3 institutions in 1 country.
Funding
Abstract
The 1,2,4-trioxolanes are a new class of synthetic peroxidic antimalarials currently in human clinical trials. The well-known reactivity of the 1,2,4-trioxolane ring toward inorganic ferrous iron and ferrous iron heme is proposed to play a role in the antimalarial action of this class of compounds. We have designed structurally relevant fluorescent chemical probes to study the subcellular localization of 1,2,4-trioxolanes in cultured Plasmodium falciparum parasites. Microscopy experiments revealed that a probe fluorescently labeled on the adamantane ring accumulated specifically in digestive vacuole-associated neutral lipid bodies within the parasite while an isosteric, but nonperoxidic, congener did not. Probes fluorescently labeled on the cyclohexane ring showed no distinct localization pattern. In their subcellular localization and peroxidative effects, 1,2,4-trioxolane probes behave much like artemisinin-based probes studied previously. Our results are consistent with a role for adamantane-derived carbon-centered radicals in the antimalarial action of 1,2,4-trioxolanes, as hypothesized previously on the basis of chemical reactivity studies.
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What OpenQuestion holds
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.