ArticleACS central science2016
Open Source Drug Discovery: Highly Potent Antimalarial Compounds Derived from the Tres Cantos Arylpyrroles.
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Article in ACS central science, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.
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29citing papers in PubMed
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Who cites it
29 citing papers in PubMed.
- Advancing global malaria control: therapeutic strategies, drug discovery, and formulation innovations.Infection · 2026Review
- Addressing infectious diseases in Africa by accelerating drug discovery through data science.Communications medicine · 2025Review
- Unravelling the mode of action of the Tres Cantos Antimalarial Set (TCAMS): investigating the mechanism of potent antimalarial compounds potentially targeting the human serotonin receptor.Malaria journal · 2025Article
- Green Synthesis of Bioactive Pyrrole DerivativesCurrent topics in medicinal chemistry · 2025Review
- Open Source Code Contributions to Global Health: The Case of Antimalarial Drug Discovery.ACS medicinal chemistry letters · 2024Article
- Open Source Antibiotics: Simple Diarylimidazoles Are Potent against Methicillin-ResistantACS infectious diseases · 2023Article
- Discovery of Novel Thiazolidinedione-Derivatives with Multi-Modal Antidiabetic Activities In Vitro and In Silico.International journal of molecular sciences · 2023Article
- Discovering New Natural Products Using Metabolomics-Based Approaches.Advances in experimental medicine and biology · 2023Article
- Target 2035 - update on the quest for a probe for every protein.RSC medicinal chemistry · 2022Article
- Functional and Material Properties in Nanocatalyst Design: A Data Handling and Sharing Problem.International journal of molecular sciences · 2021Review
- There is no market for new antibiotics: this allows an open approach to research and development.Wellcome open research · 2021Article
- Review on natural products databases: where to find data in 2020.Journal of cheminformatics · 2020Review
- Anthelmintic drug discovery: target identification, screening methods and the role of open science.Beilstein journal of organic chemistry · 2020Review
- KOBeilstein journal of organic chemistry · 2020Article
- Open Innovation in Medical and Pharmaceutical Research: A Literature Landscape Analysis.Frontiers in pharmacology · 2020Article
- Six Laws of Open Source Drug Discovery.ChemMedChem · 2019Article
- Molecular Docking Guided Grid-Independent Descriptor Analysis to Probe the Impact of Water Molecules on Conformational Changes of hERG Inhibitors in Drug Trapping Phenomenon.International journal of molecular sciences · 2019Article
- The past, present and future of anti-malarial medicines.Malaria journal · 2019Review
- Fueling Open Innovation for Malaria Transmission-Blocking Drugs: Hundreds of Molecules Targeting Early Parasite Mosquito Stages.Frontiers in microbiology · 2019Article
- Open laboratory notebooks: good for science, good for society, good for scientists.F1000Research · 2019Article
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Authors and funding
53 authors.
Alice E WilliamsonSchool of Chemistry, The University of Sydney , Sydney, New South Wales 2006, Australia.
Paul M YliojaSchool of Chemistry, The University of Sydney , Sydney, New South Wales 2006, Australia.
Murray N RobertsonSchool of Chemistry, The University of Sydney , Sydney, New South Wales 2006, Australia.
Yevgeniya Antonova-KochDepartment of Pediatrics, Pharmacology & Drug Development, University of California San Diego , 9500 Gilman Drive, La Jolla, California 92093, United States.
Vicky AveryDiscovery Biology, Eskitis Institute for Drug Discovery, Griffith University , Nathan, Queensland 4111, Australia.
Jonathan B BaellMonash Institute of Pharmaceutical Sciences, Monash University , 381 Royal Parade, Parkville, Victoria 3052, Australia.
Harikrishna BatchuCSIR-Central Drug Research Institute , Sector 10, Jankipuram Extension, Sitapur Road, Lucknow, 226 031, India.
Sanjay BatraCSIR-Central Drug Research Institute , Sector 10, Jankipuram Extension, Sitapur Road, Lucknow, 226 031, India.
Jeremy N BurrowsMedicines for Malaria Venture , PO Box 1826, 20 rte de Pre-Bois, 1215 Geneva 15, Switzerland.
Soumya BhattacharyyaCSIR-Central Drug Research Institute , Sector 10, Jankipuram Extension, Sitapur Road, Lucknow, 226 031, India.
Felix CalderonTres Cantos Medicines Development Campus, Diseases of the Developing World, GlaxoSmithKline , Severo Ochoa 2, 28760 Tres Cantos, Spain.
Susan A CharmanMonash Institute of Pharmaceutical Sciences, Monash University , 381 Royal Parade, Parkville, Victoria 3052, Australia.
Julie ClarkDepartment of Chemical Biology & Therapeutics, St. Jude Children's Research Hospital , MS 1000, Room E9050, 262 Danny Thomas Place, Memphis, Tennessee 38105-3678, United States.
Benigno CrespoTres Cantos Medicines Development Campus, Diseases of the Developing World, GlaxoSmithKline , Severo Ochoa 2, 28760 Tres Cantos, Spain.
Matin DeanSchool of Chemistry, The University of Sydney , Sydney, New South Wales 2006, Australia.
Stefan L DebbertDepartment of Chemistry, Lawrence University , 233 Steitz Science Hall, 711 East Boldt Way, Appleton, Wisconsin 54911, United States.
Michael DelvesDepartment of Life Sciences, Imperial College London , South Kensington, London SW7 2AZ, U.K.
Adelaide S M DennisResearch School of Biology, The Australian National University , Canberra, ACT 2601, Australia.
Frederik DerooseAsclepia Outsourcing Solutions , Damvalleistraat 49, B-9070 Destelbergen, Belgium.
Sandra DuffyDiscovery Biology, Eskitis Institute for Drug Discovery, Griffith University , Nathan, Queensland 4111, Australia.
Sabine FletcherDiscovery Biology, Eskitis Institute for Drug Discovery, Griffith University , Nathan, Queensland 4111, Australia.
Guri GiaeverDonnelly Centre for Cellular and Biomolecular Research, University of Toronto , 160 College Street, Toronto, Ontario M5S 3E1, Canada.
Irene HallyburtonDrug Discovery Unit, Division of Biological Chemistry and Drug Discovery, University of Dundee , Dundee, DD1 5EH, U.K.
Francisco-Javier GamoTres Cantos Medicines Development Campus, Diseases of the Developing World, GlaxoSmithKline , Severo Ochoa 2, 28760 Tres Cantos, Spain.
Marinella GebbiaDonnelly Centre for Cellular and Biomolecular Research, University of Toronto , 160 College Street, Toronto, Ontario M5S 3E1, Canada.
R Kiplin GuyDepartment of Chemical Biology & Therapeutics, St. Jude Children's Research Hospital , MS 1000, Room E9050, 262 Danny Thomas Place, Memphis, Tennessee 38105-3678, United States.
Zoe HungerfordSchool of Chemistry, The University of Sydney , Sydney, New South Wales 2006, Australia.
Kiaran KirkResearch School of Biology, The Australian National University , Canberra, ACT 2601, Australia.
Maria J Lafuente-MonasterioTres Cantos Medicines Development Campus, Diseases of the Developing World, GlaxoSmithKline , Severo Ochoa 2, 28760 Tres Cantos, Spain.
Anna LeeDonnelly Centre for Cellular and Biomolecular Research, University of Toronto , 160 College Street, Toronto, Ontario M5S 3E1, Canada.
Stephan MeisterDepartment of Pediatrics, Pharmacology & Drug Development, University of California San Diego , 9500 Gilman Drive, La Jolla, California 92093, United States.
Corey NislowDonnelly Centre for Cellular and Biomolecular Research, University of Toronto , 160 College Street, Toronto, Ontario M5S 3E1, Canada.
John P OveringtonEuropean Molecular Biology Laboratory-European Bioinformatics Institute , Wellcome Trust Genome Campus, Hinxton, Cambridgeshire CB10 1SD, U.K.
George PapadatosEuropean Molecular Biology Laboratory-European Bioinformatics Institute , Wellcome Trust Genome Campus, Hinxton, Cambridgeshire CB10 1SD, U.K.
Luc PatinyInstitute of Chemical Sciences and Engineering (ISIC), Ecole Polytechnique Fédérale de Lausanne (EPFL) , Lausanne 1015, Switzerland.
James PhamDepartment of Biochemistry & Molecular Biology, Bio21 Molecular Science and Biotechnology Institute, The University of Melbourne , Melbourne, Victoria 3010, Australia.
Stuart A RalphDepartment of Biochemistry & Molecular Biology, Bio21 Molecular Science and Biotechnology Institute, The University of Melbourne , Melbourne, Victoria 3010, Australia.
Andrea RueckerDepartment of Life Sciences, Imperial College London , South Kensington, London SW7 2AZ, U.K.
Eileen RyanMonash Institute of Pharmaceutical Sciences, Monash University , 381 Royal Parade, Parkville, Victoria 3052, Australia.
Christopher SouthanIUPHAR/BPS Guide to PHARMACOLOGY, Centre for Integrative Physiology, School of Biomedical Sciences, University of Edinburgh , Edinburgh, EH8 9XD, U.K.
Kumkum SrivastavaCSIR-Central Drug Research Institute , Sector 10, Jankipuram Extension, Sitapur Road, Lucknow, 226 031, India.
Chris SwainCambridge MedChem Consulting , 8 Mangers Lane, Duxford, Cambridge CB22 4RN, U.K.
Matthew J TarnowskiSchool of Chemistry, The University of Sydney , Sydney, New South Wales 2006, Australia.
Patrick ThomsonSchool of Chemistry, The University of Edinburgh , Joseph Black Building, West Mains Road, Edinburgh EH9 3JJ, U.K.
Peter TurnerSchool of Chemistry, The University of Sydney , Sydney, New South Wales 2006, Australia.
Iain M WallaceEuropean Molecular Biology Laboratory-European Bioinformatics Institute , Wellcome Trust Genome Campus, Hinxton, Cambridgeshire CB10 1SD, U.K.
Timothy N C WellsMedicines for Malaria Venture , PO Box 1826, 20 rte de Pre-Bois, 1215 Geneva 15, Switzerland.
Karen WhiteMonash Institute of Pharmaceutical Sciences, Monash University , 381 Royal Parade, Parkville, Victoria 3052, Australia.
Laura WhiteSchool of Chemistry, The University of Sydney , Sydney, New South Wales 2006, Australia.
Paul WillisMedicines for Malaria Venture , PO Box 1826, 20 rte de Pre-Bois, 1215 Geneva 15, Switzerland.
Elizabeth A WinzelerDepartment of Pediatrics, Pharmacology & Drug Development, University of California San Diego , 9500 Gilman Drive, La Jolla, California 92093, United States.
Sergio WittlinSwiss Tropical and Public Health Institute , Socinstrasse 57, 4051 Basel, Switzerland.
Matthew H ToddSchool of Chemistry, The University of Sydney , Sydney, New South Wales 2006, Australia.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The development of new antimalarial compounds remains a pivotal part of the strategy for malaria elimination. Recent large-scale phenotypic screens have provided a wealth of potential starting points for hit-to-lead campaigns. One such public set is explored, employing an open source research mechanism in which all data and ideas were shared in real time, anyone was able to participate, and patents were not sought. One chemical subseries was found to exhibit oral activity but contained a labile ester that could not be replaced without loss of activity, and the original hit exhibited remarkable sensitivity to minor structural change. A second subseries displayed high potency, including activity within gametocyte and liver stage assays, but at the cost of low solubility. As an open source research project, unexplored avenues are clearly identified and may be explored further by the community; new findings may be cumulatively added to the present work.
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