| Literature DB >> 21571403 |
Daniel Plano1, Ylenia Baquedano, David Moreno-Mateos, María Font, Antonio Jiménez-Ruiz, Juan Antonio Palop, Carmen Sanmartín.
Abstract
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 IC(50) 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.Entities:
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Year: 2011 PMID: 21571403 DOI: 10.1016/j.ejmech.2011.04.054
Source DB: PubMed Journal: Eur J Med Chem ISSN: 0223-5234 Impact factor: 6.514