ArticleEuropean journal of medicinal chemistry2014
Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages.
Article in European journal of medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
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Who cites it
25 citing papers in PubMed, 78 citations in OpenAlex.
- Hydroxamic Acids as HDAC Inhibitor Drug Leads for Malaria.Medicinal research reviews · 2026Review
- Screening the Global Health Priority Box against Plasmodium berghei liver stage parasites using an inexpensive luciferase detection protocol.Malaria journal · 2024Article
- PfHDAC1 is an essential regulator ofmBio · 2024Article
- Histone Deacetylase (HDAC) Inhibitors for the Treatment of Schistosomiasis.Pharmaceuticals (Basel, Switzerland) · 2022Review
- Cyclic Tetrapeptide HDAC Inhibitors with ImprovedACS infectious diseases · 2021Article
- A novel multistage antiplasmodial inhibitor targeting Plasmodium falciparum histone deacetylase 1.Cell discovery · 2020Article
- Discovery of FNDR-20123, a histone deacetylase inhibitor for the treatment of Plasmodium falciparum malaria.Malaria journal · 2020Article
- Activity of Epigenetic Inhibitors against Plasmodium falciparum Asexual and Sexual Blood Stages.Antimicrobial agents and chemotherapy · 2020Article
- Disruption of theACS infectious diseases · 2020Article
- Epigenetic reader complexes of the human malaria parasite, Plasmodium falciparum.Nucleic acids research · 2019Article
- Histone deacetylase inhibitors with high in vitro activities against Plasmodium falciparum isolates collected from Gabonese children and adults.Scientific reports · 2019Article
- Structure-Activity and Structure-Toxicity Relationships of Peptoid-Based Histone Deacetylase Inhibitors with Dual-Stage Antiplasmodial Activity.ChemMedChem · 2019Article
- 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
- HDAC inhibitor LMK‑235 promotes the odontoblast differentiation of dental pulp cells.Molecular medicine reports · 2018Article
- Insecticidal activities of histone deacetylase inhibitors against a dipteran parasite of sheep, Lucilia cuprina.International journal for parasitology. Drugs and drug resistance · 2017Article
- Bromodomains in Protozoan Parasites: Evolution, Function, and Opportunities for Drug Development.Microbiology and molecular biology reviews : MMBR · 2017Review
- Exploration of thiaheterocyclic hHDAC6 inhibitors as potential antiplasmodial agents.Future medicinal chemistry · 2017Article
- Transcriptional Profiling Defines Histone Acetylation as a Regulator of Gene Expression during Human-to-Mosquito Transmission of the Malaria ParasiteFrontiers in cellular and infection microbiology · 2017Article
- Discovery of a Selective Series of Inhibitors of Plasmodium falciparum HDACs.ACS medicinal chemistry letters · 2016Article
Corrections and comments
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Authors and funding
15 authors at 4 institutions in 4 countries.
Funding
Abstract
In this work we investigated the antiplasmodial activity of a series of HDAC inhibitors containing an alkoxyamide connecting-unit linker region. HDAC inhibitor 1a (LMK235), previously shown to be a novel and specific inhibitor of human HDAC4 and 5, was used as a starting point to rapidly construct a mini-library of HDAC inhibitors using a straightforward solid-phase supported synthesis. Several of these novel HDAC inhibitors were found to have potent in vitro activity against asexual stage Plasmodium falciparum malaria parasites. Representative compounds were shown to hyperacetylate P. falciparum histones and to inhibit deacetylase activity of recombinant PfHDAC1 and P. falciparum nuclear extracts. All compounds were also screened in vitro for activity against Plasmodium berghei exo-erythrocytic stages and selected compounds were further tested against late stage (IV and V) P. falciparum gametocytes. Of note, some compounds showed nanomolar activity against all three life cycle stages tested (asexual, exo-erythrocytic and gametocyte stages) and several compounds displayed significantly increased parasite selectivity compared to the reference HDAC inhibitor suberoylanilide hydroxamic acid (SAHA). These data suggest that it may be possible to develop HDAC inhibitors that target multiple malaria parasite life cycle stages.
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Registered trials
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