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Gold complexes with benzimidazole derivatives: synthesis,characterization and biological studies |
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| Authors: | Vinicius Zamprogno Mota Gustavo Senra Gonçalves de Carvalho Adilson David da Silva Luiz Antônio Sodré Costa Patrícia de Almeida Machado Elaine Soares Coimbra Carmen Veríssima Ferreira Silvia Mika Shishido Alexandre Cuin |
| Institution: | 1. LQBin, Laboratório de Química BioInorganica, Departamento de Química, Instituto de Ciências Exatas, Universidade Federal de Juiz de Fora, Juiz de Fora, MG, 36036-330, Brazil 2. Departamento de Química, Instituto de Ciências Exatas, Universidade Federal de Juiz de Fora, Juiz de Fora, MG, 36036-330, Brazil 3. NEQC, Núcleo de Estudos em Química Computacional, Departamento de Química, Instituto de Ciências Exatas, Universidade Federal de Juiz de Fora, Juiz de Fora, MG, 33036-330, Brazil 4. Departamento de Parasitologia, Microbiologia e Imunologia, Instituto de Ciências Biológicas, Universidade Federal de Juiz de Fora, Juiz de Fora, MG, 33036-030, Brazil 5. Laboratório de Bioensaios e Transdu??o de Sinal, Departamento de Bioquímica, Instituto de Biologia, Universidade Estadual de Campinas, Campinas, SP, 13083-862, Brazil |
| Abstract: | Synthesis, characterization, DFT studies and biological assays of new gold(I) and gold(III) complexes of benzimidazole are reported. Molecular and structural characterizations of the compounds were based on elemental (C, H and N) and thermal (TG–DTA) analyses, and FT-IR and UV–Visible spectroscopic measurements. The structures of complexes were proposed based DFT calculations. The benzimidazole compounds (Lig1 and Lig2) and the gold complexes were tested against three Leishmania species related to cutaneous manifestations of leishmaniasis. The free benzimidazole compounds showed no leishmanicidal activity. On the other hand, the gold(I and III) complexes have shown to possess significant activity against Leishmania in both stages of parasite, and the gold(III) complex with Lig2 exhibited expressive leishmanicidal activity with IC50 values below 5.7 μM. Also, the gold complexes showed high leishmania selectivity. The gold(I) complex with Lig1, for example, is almost 50 times more toxic for the parasite than for macrophages. Besides the leishmanicidal activity, all complexes exhibited toxic effect against SK-Mel 103 and Balb/c 3T3, cancer cells. |
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