Possato Bruna, Carneiro Zumira Aparecida, de Albuquerque Sérgio, Nikolaou Sofia
Departamento de Química - Faculdade de Filosofia Ciências e Letras de Ribeirão Preto da Universidade de São Paulo, Av. Bandeirantes, 3900, CEP 14040-901, Monte Alegre, Ribeirão Preto, SP, Brazil.
Faculdade de Ciências Farmacêuticas de Ribeirão Preto da Universidade de São Paulo, Av. do Café s/n, CEP: 14040-903, Monte Alegre, Ribeirão Preto, SP, Brazil.
J Inorg Biochem. 2017 Nov;176:156-158. doi: 10.1016/j.jinorgbio.2017.08.021. Epub 2017 Aug 31.
This work reports on the trypanocidal activity of a series of symmetric triruthenium complexes combined with azanaphthalene ligands of general formula [RuO(CHCOO)(L)]PF (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 IC values obtained for complexes 1-6 ranged from 1.39 to 165.9μM for the trypomastigote form and from 1.06 to 53.16μM for the amastigote form. These values were lower than the values observed for the metallic core [RuO(CHCOO)(CHOH)] itself and for the free ligands in all cases. Remarkably, complex 6 displayed lower IC 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-MK strain) and a high SI value (Selectivity Index >10) make complex 6 an excellent candidate for in vivo tests.
