Bismuth(III) complexes with 2-acetylpyridine- and 2-benzoylpyridine-derived hydrazones: Antimicrobial and cytotoxic activities and effects on the clonogenic survival of human solid tumor cells
| Autor: | Jonas Pereira Ramos, Pedro H.D.M. Prazeres, Lucas Bonfim Marques, Elaine M. Souza-Fagundes, Elisa D.L. Piló, Heloisa Beraldo, Isabella P. Ferreira, Willian R. Rocha, Angel A. Recio-Despaigne, Jacqueline A. Takahashi, Jeferson G. Da Silva |
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| Rok vydání: | 2016 |
| Předmět: |
Cell Survival
Pyridines Stereochemistry Clinical Biochemistry Pharmaceutical Science Clonogenic survival 010402 general chemistry 01 natural sciences Biochemistry Jurkat cells Colony-Forming Units Assay Inhibitory Concentration 50 Structure-Activity Relationship chemistry.chemical_compound Anti-Infective Agents Coordination Complexes Benzoylpyridinephenyl hydrazones Cell Line Tumor Neoplasms Chlorocebus aethiops Drug Discovery medicine Animals Humans Cytotoxic T cell Cytotoxicity Vero Cells Molecular Biology Bacteria Cytotoxic activity 010405 organic chemistry Organic Chemistry Hydrazones Bismuth(III) complexes Acetylpyridinephenyl hydrazones medicine.disease Antimicrobial 0104 chemical sciences Leukemia chemistry Vero cell Molecular Medicine Antibacterial activity 2-Acetylpyridine Bismuth |
| Zdroj: | LOCUS Repositório Institucional da UFV Universidade Federal de Viçosa (UFV) instacron:UFV |
| ISSN: | 0968-0896 |
| DOI: | 10.1016/j.bmc.2016.05.007 |
| Popis: | Complexes [Bi(2AcPh)Cl2]·0.5H2O (1), [Bi(2AcpClPh)Cl2] (2), [Bi(2AcpNO2Ph)Cl2] (3), [Bi(2AcpOHPh)Cl2]·2H2O (4), [Bi(H2BzPh)Cl3]·2H2O (5), [Bi(H2BzpClPh)Cl3] (6), [Bi(2BzpNO2Ph)Cl2]·2H2O (7) and [Bi(H2BzpOHPh)Cl3]·2H2O (8) were obtained with 2-acetylpyridine phenylhydrazone (H2AcPh), its -para-chloro-phenyl- (H2AcpClPh), -para-nitro-phenyl (H2AcpNO2Ph) and -para-hydroxy-phenyl (H2AcpOHPh) derivatives, as well as with the 2-benzoylpyridine phenylhydrazone analogues (H2BzPh, H2BzpClPh, H2BzpNO2Ph, H2BzpOHPh). Upon coordination to bismuth(III) antibacterial activity against Gram-positive and Gram-negative bacterial strains significantly improved except for complex (4). The cytotoxic effects of the compounds under study were evaluated on HL-60, Jurkat and THP-1 leukemia, and on MCF-7 and HCT-116 solid tumor cells, as well as on non-malignant Vero cells. In general, 2-acetylpyridine-derived hydrazones proved to be more potent and more selective as cytotoxic agents than the corresponding 2-benzoylpyridine-derived counterparts. Exposure of HCT-116 cells to H2AcpClPh, H2AcpNO2Ph and complex (3) led to 99% decrease of the clonogenic survival. The IC50 values of these compounds were three-fold smaller when cells were cultured in soft-agar (3D) than when cells were cultured in monolayer (2D), suggesting that they constitute interesting scaffolds, which should be considered in further studies aiming to develop new drug candidates for the treatment of colon cancer. |
| Databáze: | OpenAIRE |
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