Journal
JOURNAL OF INORGANIC BIOCHEMISTRY
Volume 176, Issue -, Pages 156-158Publisher
ELSEVIER SCIENCE INC
DOI: 10.1016/j.jinorgbio.2017.08.021
Keywords
Triruthenium complexes; Azanaphthalene ligands; Trypanocidal activity
Funding
- FAPESP - Fundacao de Amparo a Pesquisa do Estado de Sao Paulo [2015/20302-7, 2013/18009-4]
- CNPq - Conselho Nacional de Desenvolvimento Cientifico e Tecnologico [30415/2015-8]
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This work reports on the trypanocidal activity of a series of symmetric triruthenium complexes combined with azanaphthalene ligands of general formula [Ru3O(CH3COO)(6)(L)(3)]PF6 (L = (1) quinazoline (qui), (2) 5-nitroisoquinoline (5-nitroiq), (3) 5-bromoisoquinoline (5-briq), (4) isoquinoline (iq), (5) 5-aminoisoquinoline (5-amiq), and (6) 5,6,7,8-tetrahydroisoquinoline (thiq)). All complexes within the series presented in vitro trypanocidal activity against both the trypomastigote and amastigote forms of T. cruzi. The IC50 values obtained for complexes 1-6 ranged from 1.39 to 165.9 mu M for the trypomastigote form and from 1.06 to 53.16 mu M for the amastigote form. These values were lower than the values observed for the metallic core [Ru3O (CH3COO)(6)(CH3OH)(3)](+) itself and for the free ligands in all cases. Remarkably, complex 6 displayed lower IC50 values than the reference drug (benznidazole) for the acute (trypomastigote form) and chronic (amastigote form) phases of Chagas disease. These findings, combined with the low toxicity against healthy cells (LLK-MK2 strain) and a high SI value (Selectivity Index > 10) make complex 6 an excellent candidate for in vivo tests.
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