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

Williamson, Alice E., Ylioja, Paul M., Robertson, Murray N., Antonova, Jenya , Avery, Vicky, Baell, Jonathan, Batchu, Harikrishna, Batra, Sanjay, Burrows, Jeremy N., Bhattacharyya, Soumya, Calderon, Felix, Charman, Sue, Clark, Julie, Crespo, Benigno, Dean, Matin, Debbert, Stefan, Dennis, Adelaide S. M., Deroose, Frederik, Duffy, Sandra, Fletcher, Sabine, Giaever, Guri, Hallyburton, Irene, Gamo, Francisco-Javier, Gebbia, Marinella, Guy, R. Kiplin, Hungerford, Zoe, Kirk, Kiaran, Lafuente-Monasterio, Maria J., Lee, Anna, Meister, Stephan, Nislow, Corey, Overington, John P., Papadatos, George, Patiny, Luc, Pham, James, Ralph, Stuart, Ryan, Eileen, Southan, Chris, Svrivastava, Kumkum, Swai, Chris, Tarnowski, Matthew J., Thomson, Patrick, Turner, Peter, Wallace, Iain, Wells, Timothy N. C., White, Karen, White, Laura, Willis, Paul, Winzeler, Elizabeth A., Wittlin, Sergio and Todd, Matthew H. (2013) Open Source Drug Discovery - Highly Potent Antimalarial Compounds Derived from the GlaxoSmithKline Tres Cantos Arylpyrroles. PLoS Medicine.


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 sub-series 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 sub-series displayed high potency, including activity within a late stage gametocyte assay, 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.

Item Type: Article
Date Deposited: 27 May 2016 23:45
Last Modified: 27 May 2016 23:45


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