| Literature DB >> 21866394 |
Andressa dos Santos Portas1, Danilo Ciccone Miguel, Jenicer K U Yokoyama-Yasunaka, Silvia Reni Bortolin Uliana, Breno Pannia Espósito.
Abstract
Copper complexes with fluorinated β-diketones were synthesized and characterized in terms of lipophilicity and peroxide-assisted oxidation of dihydrorhodamine as an indicator of redox activity. The biological activity of the complexes was tested against promastigotes of Leishmania amazonensis. Inhibition of trypanosomatid-specific trypanothione reductase was also tested. It was found that the highly lipophilic and redox-active bis(trifluoroacetylacetonate) derivative had increased toxicity towards promastigotes. These results indicate that it is possible to modulate the activity of metallodrugs based on redox-active metals through the appropriate choice of lipophilic chelators in order to design new antileishmanials. Further work will be necessary to improve selectivity of these compounds against the parasite. © SBIC 2011Entities:
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Year: 2011 PMID： 21866394 DOI： 10.1007/s00775-011-0834-3
Source DB: PubMed Journal: J Biol Inorg Chem ISSN： 0949-8257 Impact factor: 3.358