ArticlePloS one2013
Anticancer properties of distinct antimalarial drug classes.
Article in PloS one, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 39 papers, 1 of them a synthesis that pooled it.
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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
39 citing papers in PubMed, 1 synthesis or guideline pooled it.
- Global research on artemisinin and its derivatives: Perspectives from patents.Pharmacological research · 2020Pooled it
- The novel amino-artemisinin derivative WHN-11 disrupts mitochondria and protein homeostasis, and induces autophagy and apoptosis in cancer cells.Scientific reports · 2025Article
- Transferrin-Conjugated Nanostructured Lipid Carriers for Targeting Artemisone to Melanoma Cells.International journal of molecular sciences · 2024Article
- Exploring Amodiaquine's Repurposing Potential in Breast Cancer Treatment-Assessment of In-Vitro Efficacy & Mechanism of Action.International journal of molecular sciences · 2022Article
- Antimalarial and antitumour activities of the steroidal quinone-methide celastrol and its combinations with artemiside, artemisone and methylene blue.Frontiers in pharmacology · 2022Article
- Artemisinin and Derivatives-Based Hybrid Compounds: Promising Therapeutics for the Treatment of Cancer and Malaria.Molecules (Basel, Switzerland) · 2021Review
- One-Pot Multicomponent Synthesis of Methoxybenzo[Molecules (Basel, Switzerland) · 2021Article
- The Anticancer Properties of Artemisia aucheri Boiss Extract on HT29 Colon Cancer Cells.Journal of gastrointestinal cancer · 2021Article
- Multistage and transmission-blocking targeted antimalarials discovered from the open-source MMV Pandemic Response Box.Nature communications · 2021Article
- Ferrous Iron-Dependent Pharmacology.Trends in pharmacological sciences · 2021Review
- A Novel 2-Carbon-Linked Dimeric Artemisinin With Potent Antileukemic Activity and Favorable Pharmacology.Frontiers in oncology · 2021Article
- Artemisinins as a novel anti-cancer therapy: Targeting a global cancer pandemic through drug repurposing.Pharmacology & therapeutics · 2020Review
- New Trends for Antimalarial Drugs: Synergism between Antineoplastics and Antimalarials on Breast Cancer Cells.Biomolecules · 2020Article
- Anticancer Activity of Pyrimethamine via Ubiquitin Mediated Degradation of AIMP2-DX2.Molecules (Basel, Switzerland) · 2020Article
- Activation of artemisinin and heme degradation in Leishmania tarentolae promastigotes: A possible link.Biochemical pharmacology · 2020Article
- RalB degradation by dihydroartemisinin induces autophagy and IFI16/caspase-1 inflammasome depression in the human laryngeal squamous cell carcinoma.Chinese medicine · 2020Article
- Anti-Melanoma Activities of Artemisone and Prenylated Amino-Artemisinins in Combination With Known Anticancer Drugs.Frontiers in pharmacology · 2020Article
- Primaquine derivatives: Modifications of the terminal amino group.European journal of medicinal chemistry · 2019Review
- Artemisinin induced reversal of EMT affects the molecular biological activity of ovarian cancer SKOV3 cell lines.Oncology letters · 2019Article
- Inhibition of Cytomegalovirus Replication with Extended-Half-Life Synthetic Ozonides.Antimicrobial agents and chemotherapy · 2019Article
Corrections and comments
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Authors and funding
10 authors.
Funding
Abstract
We have tested five distinct classes of established and experimental antimalarial drugs for their anticancer potential, using a panel of 91 human cancer lines. Three classes of drugs: artemisinins, synthetic peroxides and DHFR (dihydrofolate reductase) inhibitors effected potent inhibition of proliferation with IC50s in the nM- low µM range, whereas a DHODH (dihydroorotate dehydrogenase) and a putative kinase inhibitor displayed no activity. Furthermore, significant synergies were identified with erlotinib, imatinib, cisplatin, dasatinib and vincristine. Cluster analysis of the antimalarials based on their differential inhibition of the various cancer lines clearly segregated the synthetic peroxides OZ277 and OZ439 from the artemisinin cluster that included artesunate, dihydroartemisinin and artemisone, and from the DHFR inhibitors pyrimethamine and P218 (a parasite DHFR inhibitor), emphasizing their shared mode of action. In order to further understand the basis of the selectivity of these compounds against different cancers, microarray-based gene expression data for 85 of the used cell lines were generated. For each compound, distinct sets of genes were identified whose expression significantly correlated with compound sensitivity. Several of the antimalarials tested in this study have well-established and excellent safety profiles with a plasma exposure, when conservatively used in malaria, that is well above the IC50s that we identified in this study. Given their unique mode of action and potential for unique synergies with established anticancer drugs, our results provide a strong basis to further explore the potential application of these compounds in cancer in pre-clinical or and clinical settings.
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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.