3-Alkylthio-1,2,4-triazine dimers with potent antimalarial activity |
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Authors: | Kung Ban Sandra Duffy Yelena Khakham Vicky M Avery Andrew Hughes Oliver Montagnat Kasiram Katneni Eileen Ryan Jonathan B Baell |
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Institution: | 1. Walter & Eliza Hall Institute of Medical Research, Parkville, Victoria, Australia;2. Eskitis Institute for Cell and Molecular Therapies, Griffith University, Nathan, Queensland, Australia;3. La Trobe University, Bundoora, Victoria, Australia;4. Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University (Parkville Campus), Victoria, Australia |
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Abstract: | We report on the discovery of 3-alkylthio-1,2,4-triazine dimers that are potently toxic to Plasmodium falciparum, with single digit nanomolar activity, and up to several thousand-fold lower toxicity to mammalian cells. They are equipotent against chloroquine-resistant strains of P. falciparum. |
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