Open Source Drug Discovery: Highly Potent Antimalarial Compounds Derived from the Tres Cantos Arylpyrroles

Author:

Williamson Alice E.1,Ylioja Paul M.1,Robertson Murray N.1,Antonova-Koch Yevgeniya2,Avery Vicky3,Baell Jonathan B.4,Batchu Harikrishna5,Batra Sanjay5,Burrows Jeremy N.6,Bhattacharyya Soumya5,Calderon Felix7,Charman Susan A.4,Clark Julie8,Crespo Benigno7,Dean Matin1,Debbert Stefan L.9,Delves Michael10,Dennis Adelaide S. M.11,Deroose Frederik12,Duffy Sandra3,Fletcher Sabine3,Giaever Guri13,Hallyburton Irene14,Gamo Francisco-Javier7,Gebbia Marinella13,Guy R. Kiplin8,Hungerford Zoe1,Kirk Kiaran11,Lafuente-Monasterio Maria J.7,Lee Anna13,Meister Stephan2,Nislow Corey13,Overington John P.15,Papadatos George15,Patiny Luc16,Pham James17,Ralph Stuart A.17,Ruecker Andrea10,Ryan Eileen4,Southan Christopher18,Srivastava Kumkum5,Swain Chris19,Tarnowski Matthew J.1,Thomson Patrick20,Turner Peter1,Wallace Iain M.15,Wells Timothy N. C.6,White Karen4,White Laura1,Willis Paul6,Winzeler Elizabeth A.2,Wittlin Sergio21,Todd Matthew H.1

Affiliation:

1. School of Chemistry, The University of Sydney, Sydney, New South Wales 2006, Australia

2. Department of Pediatrics, Pharmacology & Drug Development, University of California San Diego, 9500 Gilman Drive, La Jolla, California 92093, United States

3. Discovery Biology, Eskitis Institute for Drug Discovery, Griffith University, Nathan, Queensland 4111, Australia

4. Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, Parkville, Victoria 3052, Australia

5. CSIR-Central Drug Research Institute, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow, 226 031, India

6. Medicines for Malaria Venture, PO Box 1826, 20 rte de Pre-Bois, 1215 Geneva 15, Switzerland

7. Tres Cantos Medicines Development Campus, Diseases of the Developing World, GlaxoSmithKline, Severo Ochoa 2, 28760 Tres Cantos, Spain

8. Department of Chemical Biology & Therapeutics, St. Jude Children’s Research Hospital, MS 1000, Room E9050, 262 Danny Thomas Place, Memphis, Tennessee 38105-3678, United States

9. Department of Chemistry, Lawrence University, 233 Steitz Science Hall, 711 East Boldt Way, Appleton, Wisconsin 54911, United States

10. Department of Life Sciences, Imperial College London, South Kensington, London SW7 2AZ, U.K.

11. Research School of Biology, The Australian National University, Canberra, ACT 2601, Australia

12. Asclepia Outsourcing Solutions, Damvalleistraat 49, B-9070 Destelbergen, Belgium

13. Donnelly Centre for Cellular and Biomolecular Research, University of Toronto, 160 College Street, Toronto, Ontario M5S 3E1, Canada

14. Drug Discovery Unit, Division of Biological Chemistry and Drug Discovery, University of Dundee, Dundee, DD1 5EH, U.K.

15. European Molecular Biology Laboratory—European Bioinformatics Institute, Wellcome Trust Genome Campus, Hinxton, Cambridgeshire CB10 1SD, U.K.

16. Institute of Chemical Sciences and Engineering (ISIC), Ecole Polytechnique Fédérale de Lausanne (EPFL), Lausanne 1015, Switzerland

17. Department of Biochemistry & Molecular Biology, Bio21 Molecular Science and Biotechnology Institute, The University of Melbourne, Melbourne, Victoria 3010, Australia

18. IUPHAR/BPS Guide to PHARMACOLOGY, Centre for Integrative Physiology, School of Biomedical Sciences, University of Edinburgh, Edinburgh, EH8 9XD, U.K.

19. Cambridge MedChem Consulting, 8 Mangers Lane, Duxford, Cambridge CB22 4RN, U.K.

20. School of Chemistry, The University of Edinburgh, Joseph Black Building, West Mains Road, Edinburgh EH9 3JJ, U.K.

21. Swiss Tropical and Public Health Institute, Socinstrasse 57, 4051 Basel, Switzerland

Funder

University Of Edinburgh

National Health and Medical Research Council

Australian Research Council

Wellcome Trust

Medicines for Malaria Venture

European Molecular Biology Laboratory

Publisher

American Chemical Society (ACS)

Subject

General Chemical Engineering,General Chemistry

Reference124 articles.

1. WHO. World Malaria Report 2015,http://www.who.int/malaria/publications/world-malaria-report-2015/en/, accessed March 15, 2016.

2. Snow, R. W., Craig, M., Newton, C., and Steketee, R.The Public Health Burden of Plasmodium falciparum Malaria in Africa: Deriving the Numbers;Fogarty International Centre, National Institutes of Health:Bethesda, MD, 2010, 1–81.

3. The Global Malaria Action Plan, Geneva,2008,http://www.rollbackmalaria.org/microsites/gmap/, accessed Dec 8, 2015.

4. Changes in the Treatment Responses to Artesunate-Mefloquine on the Northwestern Border of Thailand during 13 Years of Continuous Deployment

5. Artemisinin Resistance inPlasmodium falciparumMalaria

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