ArticleEuropean journal of medicinal chemistry2023
Discovery of potent Plasmodium falciparum protein kinase 6 (PfPK6) inhibitors with a type II inhibitor pharmacophore.
Article in European journal of medicinal chemistry, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed.
- Using Unbiased Chemical Proteomics Approaches to Explore the Target Landscape of the Resistance Refractory 7-Azaindole MMV022224 inACS infectious diseases · 2026Article
- Computationally guided optimization of the antimalarial activity and physicochemical properties of 2,4-diaminopyrimidines.RSC medicinal chemistry · 2025Article
- Advancing antimalarial drug discovery: ensemble machine learning models for predicting PfPK6 inhibitor activity.Molecular diversity · 2025Article
- Plasmodiumfalciparum protein kinase 6 and hemozoin formation are inhibited by a type II human kinase inhibitor exhibiting antimalarial activity.Cell chemical biology · 2025Article
- Towards next-generation treatment options to combat Plasmodium falciparum malaria.Nature reviews. Microbiology · 2025Review
- Discovery of Potent Antimalarial Type II Kinase Inhibitors with Selectivity over Human Kinases.Journal of medicinal chemistry · 2024Article
- Characterization of 2,4-Dianilinopyrimidines Against FiveACS medicinal chemistry letters · 2023Article
- How many kinases are druggable? A review of our current understanding.The Biochemical journal · 2023Article
- Roles of Virtual Screening and Molecular Dynamics Simulations in Discovering and Understanding Antimalarial Drugs.International journal of molecular sciences · 2023Review
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Authors and funding
15 authors.
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Abstract
Malaria is a devastating disease that causes significant global morbidity and mortality. The rise of drug resistance against artemisinin-based combination therapy demonstrates the necessity to develop alternative antimalarials with novel mechanisms of action. We report the discovery of Ki8751 as an inhibitor of essential kinase PfPK6. 79 derivatives were designed, synthesized and evaluated for PfPK6 inhibition and antiplasmodial activity. Using group efficiency analyses, we established the importance of key groups on the scaffold consistent with a type II inhibitor pharmacophore. We highlight modifications on the tail group that contribute to antiplasmodial activity, cumulating in the discovery of compound 67, a PfPK6 inhibitor (IC
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