ArticleACS medicinal chemistry letters2016
Discovery of a Selective Series of Inhibitors of Plasmodium falciparum HDACs.
Article in ACS medicinal chemistry letters, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 40 citations in OpenAlex.
- Hydroxamic Acids as HDAC Inhibitor Drug Leads for Malaria.Medicinal research reviews · 2026Review
- Efficient and metal catalyst-free approach towards highly-substituted N-sulfonylpiperidine-/mono-spiro-1,2,4,5-tetraoxanes for potential applications in chemotherapy.Scientific reports · 2026Article
- Exploring Alternative Zinc-Binding Groups in Histone Deacetylase (HDAC) Inhibitors UncoversJournal of medicinal chemistry · 2025Article
- Epigenetic regulation as a therapeutic target in the malaria parasite Plasmodium falciparum.Malaria journal · 2024Review
- 1,3-Diphenylureido hydroxamate as a promising scaffold for generation of potent antimalarial histone deacetylase inhibitors.Scientific reports · 2023Article
- Synthesis, Antiplasmodial, and Antileukemia Activity of Dihydroartemisinin-HDAC Inhibitor Hybrids as Multitarget Drugs.Pharmaceuticals (Basel, Switzerland) · 2022Article
- Histone Deacetylase (HDAC) Inhibitors for the Treatment of Schistosomiasis.Pharmaceuticals (Basel, Switzerland) · 2022Review
- Antimalarial Inhibitors Targeting Epigenetics or Mitochondria inMolecules (Basel, Switzerland) · 2021Review
- An ELISA method to assess HDAC inhibitor-induced alterations to P. falciparum histone lysine acetylation.International journal for parasitology. Drugs and drug resistance · 2020Article
- Discovery of FNDR-20123, a histone deacetylase inhibitor for the treatment of Plasmodium falciparum malaria.Malaria journal · 2020Article
- Epigenetic inhibitors target multiple stages of Plasmodium falciparum parasites.Scientific reports · 2020Article
- Improved Selective Class I HDAC and Novel Selective HDAC3 Inhibitors: Beyond Hydroxamic Acids and Benzamides.ACS medicinal chemistry letters · 2019Article
- Identification of novel multi-stage histone deacetylase (HDAC) inhibitors that impair Schistosoma mansoni viability and egg production.Parasites & vectors · 2018Article
- One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites.European journal of medicinal chemistry · 2018Article
- In silico identification of inhibitors against Plasmodium falciparum histone deacetylase 1 (PfHDAC-1).Journal of molecular modeling · 2018Article
- Design, Synthesis, and Biological Evaluation of the First c-Met/HDAC Inhibitors Based on Pyridazinone Derivatives.ACS medicinal chemistry letters · 2017Article
- Exploration of thiaheterocyclic hHDAC6 inhibitors as potential antiplasmodial agents.Future medicinal chemistry · 2017Article
Corrections and comments
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Authors and funding
22 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The identification of a new series of P. falciparum growth inhibitors is described. Starting from a series of known human class I HDAC inhibitors a SAR exploration based on growth inhibitory activity in parasite and human cells-based assays led to the identification of compounds with submicromolar inhibition of P. falciparum growth (EC50 < 500 nM) and good selectivity over the activity of human HDAC in cells (up to >50-fold). Inhibition of parasital HDACs as the mechanism of action of this new class of selective growth inhibitors is supported by hyperacetylation studies.
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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.