2011
DOI: 10.1371/journal.pntd.0001412
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Integrated Dataset of Screening Hits against Multiple Neglected Disease Pathogens

Abstract: New chemical entities are desperately needed that overcome the limitations of existing drugs for neglected diseases. Screening a diverse library of 10,000 drug-like compounds against 7 neglected disease pathogens resulted in an integrated dataset of 744 hits. We discuss the prioritization of these hits for each pathogen and the strong correlation observed between compounds active against more than two pathogens and mammalian cell toxicity. Our work suggests that the efficiency of early drug discovery for negle… Show more

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Cited by 52 publications
(43 citation statements)
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“…Extracellular form (epimastigote) is the most commonly used owing to its easy culture in laboratory, but tests obtained on intracellular amastigotes (responsible for the chronic phase of CD) and blood trypomastigotes are more indicative due to these form of the parasite is the developed form in vertebrate hosts 23 . According to some authors, for deeming a compound as potential antichagasic agent, it has to meet certain criteria 24 . In the first place, the IC 50 value has to be around 10 µM and the in second place the SI has to be 50 times higher than that of the reference drug.…”
Section: Resultsmentioning
confidence: 99%
“…Extracellular form (epimastigote) is the most commonly used owing to its easy culture in laboratory, but tests obtained on intracellular amastigotes (responsible for the chronic phase of CD) and blood trypomastigotes are more indicative due to these form of the parasite is the developed form in vertebrate hosts 23 . According to some authors, for deeming a compound as potential antichagasic agent, it has to meet certain criteria 24 . In the first place, the IC 50 value has to be around 10 µM and the in second place the SI has to be 50 times higher than that of the reference drug.…”
Section: Resultsmentioning
confidence: 99%
“…The initial aim of the Malaria Box was to catalyze research into malaria and the discovery of new antimalarial clinical candidates. However, the utility of the Malaria Box goes beyond the malaria field since these biologically active, cell permeable compounds are highly likely to be active against other parasitic or neglected diseases [30],[31]. The overlap between the biologies of the basic apicocomplexan parasites suggests that hits from malaria screens would be useful against leishmaniasis and trypanosomiasis, and even on helminth targets [30].…”
Section: Discussionmentioning
confidence: 99%
“…All series which were not cidal, or which had been the subject of previously reported studies, were subsequently excluded. 2531 The screening cascade is shown in Figure 1. 22 …”
Section: Hit Discoverymentioning
confidence: 99%