Gold complexes with benzimidazole derivatives: synthesis, characterization and biological studies
| Autor: | Silvia Mika Shishido, Alexandre Cuin, Elaine Soares Coimbra, Luiz Antônio S. Costa, Carmen Veríssima Ferreira, Patrícia A. Machado, Adilson David da Silva, Vinicius Zamprogno Mota, Gustavo S.G. de Carvalho |
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| Rok vydání: | 2013 |
| Předmět: |
Benzimidazole
Stereochemistry Antiprotozoal Agents Antineoplastic Agents General Biochemistry Genetics and Molecular Biology Biomaterials chemistry.chemical_compound Mice Structure-Activity Relationship Ic50 values Molecule Structure–activity relationship Animals Humans Cytotoxicity Cells Cultured Cell Proliferation Leishmania Mice Inbred BALB C Biological studies biology Dose-Response Relationship Drug Molecular Structure Chemistry Macrophages Metals and Alloys 3T3 Cells biology.organism_classification Quantum Theory Benzimidazoles Drug Screening Assays Antitumor General Agricultural and Biological Sciences Selectivity Organogold Compounds |
| Zdroj: | Biometals : an international journal on the role of metal ions in biology, biochemistry, and medicine. 27(1) |
| ISSN: | 1572-8773 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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