Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 46, Issue 8, Pages 3315-3323Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2011.04.054
Keywords
Selenocyanate; Diselenide; Antileishmanial activity
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Funding
- University of Navarra Research Plan (Plan de Investigacion de la Universidad de Navarra, PIUNA)
- CAN Foundation
- Ministerio de Educacion y Ciencia, Spain [SAF 2009-13914-CO2-02]
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Thirty five selenocyanate and diselenide compounds were subjected to in vitro screening against Leishmania infantum promastigotes and the most active ones were also tested in an axenic amastigote model. In order to establish the selectivity indexes (SI) the cytotoxic effect of each compound was also assayed against Jurkat and THP-1 cell lines. Thirteen derivatives exhibit better IC50 values than miltefosine and edelfosine. Bis(4-aminophenyl) diselenide exhibits the best activity when assayed in infected macrophages and one of the lowest cytotoxic activities against the human cell lines tested, with SI values of 32 and 24 against Jurkat and THP-1 cells, respectively. This compound thus represents a new lead for further studies aimed at establishing its mechanism of action. (C) 2011 Elsevier Masson SAS. All rights reserved.
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