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In vitro activity of BNIP derivatives.

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posted on 2018-01-22, 18:31 authored by Luís Gaspar, Ross P. Coron, Paul KongThoo Lin, David M. Costa, Begoña Perez-Cabezas, Joana Tavares, Meritxell Roura-Ferrer, Isbaal Ramos, Céline Ronin, Louise L. Major, Fabrice Ciesielski, Iain K. Pemberton, Jane MacDougall, Paola Ciapetti, Terry K. Smith, Anabela Cordeiro-da-Silva

A) Primary screening of BNIP derivatives by an in vitro assay for intracellular T. cruzi amastigotes at a single dose of 2.5 μM. Values for both anti-parasitic activity and cell ratio are represented in the dot plot graph. The blue square represents the zone of selection for active, low toxicity hits to be evaluated by dose-response curve analysis. The green square represents the zone of selection for compounds to be tested at a higher dose. B) Primary screening of the compounds selected for testing at a higher dose of 10 μM. Values for both anti-parasitic activity and cell ratio are represented in the dot plot graph. The blue square represents the zone of selection for active, low toxicity hits to be evaluated by dose-response curve analysis. C) Representation of the selectivity indexes of the compounds analysed by dose-response curve analysis, with the determined anti-parasitic activity (EC50) in the y axis, and the cell ratio (CC50) in the x axis. Dots represent the average of three independent experiments.

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