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Selenocyanates and diselenides: A new class of potent antileishmanial agents

2011; Elsevier BV; Volume: 46; Issue: 8 Linguagem: Inglês

10.1016/j.ejmech.2011.04.054

1768-3254

Daniel Plano, Ylenia Baquedano, David Moreno-Mateos, Marı́a Font, Antonio Jiménez-Ruı́z, Juan Antonio Palop, Carmen Sanmartín,

Insect and Pesticide Research

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.