ArticleJournal of medicinal chemistry2011
Discovery of novel alkylated (bis)urea and (bis)thiourea polyamine analogues with potent antimalarial activities.
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 29 papers.
What it found
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Who cites it
29 citing papers in PubMed, 97 citations in OpenAlex.
- Synthesis and SAR Studies of Acyl-Thiourea Platinum(II) Complexes Yield Analogs with Dual-Stage Antiplasmodium Activity.ACS medicinal chemistry letters · 2025Article
- Eliminating malaria transmission requires targeting immature and mature gametocytes through lipoidal uptake of antimalarials.Nature communications · 2024Article
- Patrick M. Woster Memorial Commentary.ACS medicinal chemistry letters · 2023Article
- Antiprotozoal Activity of Benzoylthiourea Derivatives againstPathogens (Basel, Switzerland) · 2023Article
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- Synthesis and Testing of Analogs of the Tuberculosis Drug Candidate SQ109 against Bacteria and Protozoa: Identification of Lead Compounds againstACS infectious diseases · 2023Article
- New Transmission-Selective Antimalarial Agents through Hit-to-Lead Optimization of 2-([1,1'-Biphenyl]-4-carboxamido)benzoic Acid Derivatives.Chembiochem : a European journal of chemical biology · 2022Article
- Antimalarial and antitumour activities of the steroidal quinone-methide celastrol and its combinations with artemiside, artemisone and methylene blue.Frontiers in pharmacology · 2022Article
- The Artemiside-Artemisox-Artemisone-M1 Tetrad: Efficacies against Blood StagePharmaceutics · 2021Article
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- Naphthylisoquinoline alkaloids, validated as hit multistage antiplasmodial natural products.International journal for parasitology. Drugs and drug resistance · 2020Article
- Urea Derivatives in Modern Drug Discovery and Medicinal Chemistry.Journal of medicinal chemistry · 2020Article
- Epigenetic inhibitors target multiple stages of Plasmodium falciparum parasites.Scientific reports · 2020Article
- Unforeseen Possibilities To Investigate the Regulation of Polyamine Metabolism Revealed by Novel C-Methylated Spermine Derivatives.Journal of medicinal chemistry · 2019Article
- Bioassay-guided isolation and identification of gametocytocidal compounds from Artemisia afra (Asteraceae).Malaria journal · 2019Article
- Optimal 10-Aminoartemisinins With Potent Transmission-Blocking Capabilities for New Artemisinin Combination Therapies-Activities Against Blood StageFrontiers in chemistry · 2019Article
- Novel Synthetic Polyamines Have Potent Antimalarial ActivitiesFrontiers in cellular and infection microbiology · 2019Article
- Artemisone and Artemiside Are Potent Panreactive Antimalarial Agents That Also Synergize Redox Imbalance in Plasmodium falciparum Transmissible Gametocyte Stages.Antimicrobial agents and chemotherapy · 2018Article
- Antibacterial Diamines Targeting Bacterial Membranes.Journal of medicinal chemistry · 2016Article
Corrections and comments
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Authors and funding
7 authors at 3 institutions in 2 countries.
Funding
Abstract
A series of alkylated (bis)urea and (bis)thiourea polyamine analogues were synthesized and screened for antimalarial activity against chloroquine-sensitive and -resistant strains of Plasmodium falciparum in vitro. All analogues showed growth inhibitory activity against P. falciparum at less than 3 μM, with the majority having effective IC(50) values in the 100-650 nM range. Analogues arrested parasitic growth within 24 h of exposure due to a block in nuclear division and therefore asexual development. Moreover, this effect appears to be cytotoxic and highly selective to malaria parasites (>7000-fold lower IC(50) against P. falciparum) and is not reversible by the exogenous addition of polyamines. With this first report of potent antimalarial activity of polyamine analogues containing 3-7-3 or 3-6-3 carbon backbones and substituted terminal urea- or thiourea moieties, we propose that these compounds represent a structurally novel class of antimalarial agents.
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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.