ArticleChemMedChem2015
Drug delivery to the malaria parasite using an arterolane-like scaffold.
Article in ChemMedChem, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 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
19 citing papers in PubMed.
- Toward Tumor-Conditional Release of Histone Deacetylase Inhibitors from Nongenotoxic Drug Conjugates.ACS medicinal chemistry letters · 2026Article
- Three decades of selective product formationRSC advances · 2025Review
- Elevated labile iron in castration-resistant prostate cancer is targetable with ferrous iron-activatable antiandrogen therapy.European journal of medicinal chemistry · 2023Article
- Synthesis and in vitro Study of Artemisinin/Synthetic Peroxide-Based Hybrid Compounds against SARS-CoV-2 and Cancer.ChemMedChem · 2022Article
- Lewis Acids and Heteropoly Acids in the Synthesis of Organic Peroxides.Pharmaceuticals (Basel, Switzerland) · 2022Review
- Expanded scope of Griesbaum co-ozonolysis for the preparation of structurally diverse sensors of ferrous iron.RSC advances · 2021Article
- Emerging role of ferrous iron in bacterial growth and host-pathogen interaction: New tools for chemical (micro)biology and antibacterial therapy.Current opinion in chemical biology · 2021Review
- Ferrous Iron-Dependent Pharmacology.Trends in pharmacological sciences · 2021Review
- Multi-omic Characterization of the Mode of Action of a Potent New Antimalarial Compound, JPC-3210, AgainstMolecular & cellular proteomics : MCP · 2020Article
- Inorganic Chemistry Approaches to Activity-Based Sensing: From Metal Sensors to Bioorthogonal Metal Chemistry.Inorganic chemistry · 2019Review
- Targeting Mobilization of Ferrous Iron inACS infectious diseases · 2019Article
- Versatile Histochemical Approach to Detection of Hydrogen Peroxide in Cells and Tissues Based on Puromycin Staining.Journal of the American Chemical Society · 2018Article
- New endoperoxides highly active in vivo and in vitro against artemisinin-resistant Plasmodium falciparum.Malaria journal · 2018Article
- Activity-based sensing fluorescent probes for iron in biological systems.Current opinion in chemical biology · 2018Review
- A Novel Tumor-Activated Prodrug Strategy Targeting Ferrous Iron Is Effective in Multiple Preclinical Cancer Models.Journal of medicinal chemistry · 2016Article
- An Endoperoxide Reactivity-Based FRET Probe for Ratiometric Fluorescence Imaging of Labile Iron Pools in Living Cells.Journal of the American Chemical Society · 2016Article
- A reactivity-based probe of the intracellular labile ferrous iron pool.Nature chemical biology · 2016Article
- Trioxolane-Mediated Delivery of Mefloquine Limits Brain Exposure in a Mouse Model of Malaria.ACS medicinal chemistry letters · 2015Article
- Efficient and stereocontrolled synthesis of 1,2,4-trioxolanes useful for ferrous iron-dependent drug delivery.Organic letters · 2014Article
Corrections and comments
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Authors and funding
6 authors.
Funding
Abstract
Antimalarial agents artemisinin and arterolane act via initial reduction of a peroxide bond in a process likely mediated by ferrous iron sources in the parasite. Here, we report the synthesis and antiplasmodial activity of arterolane-like 1,2,4-trioxolanes specifically designed to release a tethered drug species within the malaria parasite. Compared with our earlier drug delivery scaffolds, these new arterolane-inspired systems are of significantly decreased molecular weight and possess superior metabolic stability. We describe an efficient, concise and scalable synthesis of the new systems, and demonstrate the use of the aminonucleoside antibiotic puromycin as a chemo/biomarker to validate successful drug release in live Plasmodium falciparum parasites. Together, the improved drug-like properties, more efficient synthesis, and proof of concept using puromycin, suggests these new molecules as improved vehicles for targeted drug delivery to the malaria parasite.
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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.