ReviewCurrent topics in medicinal chemistry2012
Back to the future: lessons learned in modern target-based and whole-cell lead optimization of antimalarials.
Review in Current topics in medicinal chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed.
- Chiral Monoamidines as Effective Organocatalysts for the Stereoselective Synthesis of Oxindoles under Homogeneous and Heterogeneous Conditions.The Journal of organic chemistry · 2025Article
- Current status of experimental models for the study of malaria.Parasitology · 2022Review
- Modern Approaches in the Discovery and Development of Plant-Based Natural Products and Their Analogues as Potential Therapeutic Agents.Molecules (Basel, Switzerland) · 2022Review
- Transporter-Mediated Solutes Uptake as Drug Target inFrontiers in pharmacology · 2022Review
- Actives from MMV Open Access Boxes? A suggested way forward.PLoS pathogens · 2021Review
- QSAR-Based Virtual Screening of Natural Products Database for Identification of Potent Antimalarial Hits.Biomolecules · 2021Article
- Virtual-screening workflow tutorials and prospective results from the Teach-Discover-Treat competition 2014 against malaria.F1000Research · 2017Article
- The malaria parasite cation ATPase PfATP4 and its role in the mechanism of action of a new arsenal of antimalarial drugs.International journal for parasitology. Drugs and drug resistance · 2015Review
- (+)-SJ733, a clinical candidate for malaria that acts through ATP4 to induce rapid host-mediated clearance of Plasmodium.Proceedings of the National Academy of Sciences of the United States of America · 2014Article
- The discovery of first-in-class drugs: origins and evolution.Nature reviews. Drug discovery · 2014Review
- Pharmacokinetics, metabolism, andACS medicinal chemistry letters · 2013Article
- Recent advances in malaria drug discovery.Bioorganic & medicinal chemistry letters · 2013Review
- Prediction of the P. falciparum target space relevant to malaria drug discovery.PLoS computational biology · 2013Article
- Stoking the drug target pipeline for human African trypanosomiasis.Molecular microbiology · 2012Article
Corrections and comments
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Authors and funding
2 authors.
Funding
Abstract
Antimalarial drug discovery has historically benefited from the whole-cell (phenotypic) screening approach to identify lead molecules in the search for new drugs. However over the past two decades there has been a shift in the pharmaceutical industry to move away from whole-cell screening to target-based approaches. As part of a Wellcome Trust and Medicines for Malaria Venture (MMV) funded consortium to discover new blood-stage antimalarials, we used both approaches to identify new antimalarial chemotypes, two of which have progressed beyond the lead optimization phase and display excellent in vivo efficacy in mice. These two advanced series were identified through a cell-based optimization devoid of target information and in this review we summarize the advantages of this approach versus a target-based optimization. Although the each lead optimization required slightly different medicinal chemistry strategies, we observed some common issues across the different the scaffolds which could be applied to other cell based lead optimization programs.
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Registered trials
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