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Your search keyword '"Gabrieli L. Parrilha"' showing total 3 results
Start Over Author "Gabrieli L. Parrilha" Journal european journal of medicinal chemistry
3 results on '"Gabrieli L. Parrilha"'

1. Pyridine-derived thiosemicarbazones and their tin(IV) complexes with antifungal activity against Candida spp

Author

Nivaldo L. Speziali, Roberta P. Dias, Ludmila Ferreira Gouveia, Alan Kiill Gasparoto, Heloisa Beraldo, Jeferson G. Da Silva, Daniel Assis Santos, Gabrieli L. Parrilha, and Willian R. Rocha

Subjects
Models, Molecular, Thiosemicarbazones, Antifungal Agents, Pyridines, Stereochemistry, Microbial Sensitivity Tests, Crystallography, X-Ray, Candida parapsilosis, Structure-Activity Relationship, chemistry.chemical_compound, Minimum inhibitory concentration, Candida krusei, Drug Discovery, Organometallic Compounds, medicine, Candida albicans, Semicarbazone, Candida, Pharmacology, Molecular Structure, biology, Candida glabrata, Organic Chemistry, Stereoisomerism, General Medicine, biology.organism_classification, Corpus albicans, chemistry, Tin, Fluconazole, medicine.drug
Abstract

[(n-Bu)Sn(2Ac4oClPh)Cl2] (1), [(n-Bu)Sn(2Ac4oFPh)Cl2] (2), [(n-Bu)Sn(2Ac4oNO2Ph)Cl2] (3), [(n-Bu)Sn(2Bz4oClPh)Cl2] (4), [(n-Bu)Sn(2Bz4oFPh)Cl2] (5) and [(n-Bu)Sn(2Bz4oNO2Ph)Cl2] (6) were obtained by reacting [(n-Bu)SnCl3] with 2-acetylpyridine-N4-orthochlorophenyl thiosemicarbazone (H2Ac4oClPh), 2-acetylpyridine-N4-orthofluorphenyl thiosemicarbazone (H2Ac4oFPh), 2-acetylpyridine-N4-orthonitrophenyl thiosemicarbazone (H2Ac4oNO2Ph), and with the corresponding 2-benzoylpyridine-derived thiosemicarbazones (H2Bz4oClPh, H2ABz4oFPh and H2Bz4oNO2Ph). The antifungal activity of the studied compounds was evaluated against several Candida species. Upon coordination of H2Bz4oNO2Ph to tin in complex (6) the antifungal activity increased three times against Candida albicans and Candida krusei and six times against Candida glabrata and Candida parapsilosis. The minimum inhibitory concentration (MIC) values of H2Ac4oNO2Ph and its complex (3) against C. albicans, C. parapsilosis and C. glabrata are similar to that of fluconazole. All studied compounds were more active than fluconazole against C. krusei.

Published
2011
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2. Metal complexes with 2-acetylpyridine-N(4)-orthochlorophenylthiosemicarbazone: cytotoxicity and effect on the enzymatic activity of thioredoxin reductase and glutathione reductase

Author

Josane A. Lessa, Jonas Pereira Ramos, Ingo Ott, Bernardo L. Rodrigues, Karina S.O. Ferraz, Elaine M. Souza-Fagundes, Heloisa Beraldo, Gabrieli L. Parrilha, and Kely Navakoski de Oliveira

Subjects
Models, Molecular, Thiosemicarbazones, Thioredoxin-Disulfide Reductase, Stereochemistry, Cell Survival, Thioredoxin reductase, Glutathione reductase, Metal, chemistry.chemical_compound, Structure-Activity Relationship, Coordination Complexes, Drug Discovery, Chlorocebus aethiops, Organometallic Compounds, Animals, Humans, Enzyme Inhibitors, Cytotoxicity, Semicarbazone, Vero Cells, Pharmacology, chemistry.chemical_classification, biology, Dose-Response Relationship, Drug, Molecular Structure, Organic Chemistry, Selenol, Active site, General Medicine, Rats, Enzyme, Glutathione Reductase, chemistry, Biochemistry, Liver, visual_art, visual_art.visual_art_medium, biology.protein, MCF-7 Cells, HT29 Cells
Abstract

Metal complexes with 2-acetylpyridine-N(4)-orthochlorophenylthiosemicarbazone (H2Ac4oClPh) were assayed for their cytotoxicity against MCF-7 breast adenocarcinoma and HT-29 colon carcinoma cells. The thiosemicarbazone and most of the complexes were highly cytotoxic. H2Ac4oClPh and its gallium(III) and tin(IV) complexes did not show any inhibitory activity against thioredoxin reductase (TrxR) and glutathione reductase (GR). The palladium(II), platinum(II) and bismuth(III) complexes inhibited TrxR at micromolar concentrations but not GR. The antimony(III) and gold(III) complexes strongly inhibited TrxR at submicromolar doses with GR inhibition at higher concentrations. The selectivity of these complexes for TrxR suggests metal binding to a selenol residue in the active site of the enzyme. TrxR inhibition is likely a contributing factor to the mode of action of the gold and antimony derivatives.

Published
2014

3. 2-Acetylpyridine- and 2-benzoylpyridine-derived hydrazones and their gallium(III) complexes are highly cytotoxic to glioma cells

Author

Oscar E. Piro, Angel A. Recio Despaigne, Jans B. Izidoro, Eduardo E. Castellano, Pryscila R. da Costa, Raquel Gouvêa dos Santos, Gabrieli L. Parrilha, Heloisa Beraldo, and Willian R. Rocha

Subjects
Models, Molecular, Pyridines, Mutant, chemistry.chemical_element, Quantitative Structure-Activity Relationship, Antineoplastic Agents, Apoptosis, Gallium, Crystallography, X-Ray, chemistry.chemical_compound, Fetus, Glioma, Drug Discovery, medicine, Ic50 values, Cytotoxic T cell, Humans, Fibroblast, neoplasms, Lung, Cells, Cultured, Cell Proliferation, Pharmacology, Molecular Structure, Brain Neoplasms, Organic Chemistry, Hydrazones, General Medicine, Fibroblasts, PROTEÍNAS, medicine.disease, nervous system diseases, medicine.anatomical_structure, chemistry, Biochemistry, Human fetal, 2-Acetylpyridine
Abstract

2-Acetylpyridine-phenylhydrazone (H2AcPh), its para-chlorophenylhydrazone (H2AcpClPh) and para-nitrophenylhydrazone (H2AcpNO2Ph) analogues, the corresponding 2-benzoylpyridine-derived hydrazones (H2BzPh, H2BzpClPh and H2BzpNO2Ph) and their gallium(III) complexes were assayed for their cytotoxic activity against U87 (expressing wild-type p53 protein) and T98 (expressing mutant p53 protein) glioma cells. IC50 values against both glioma cells and against the MRC5 (human fetal lung fibroblast) lineage were obtained for the hydrazones, but not for their gallium(III) complexes, due to their low solubility. Hydrazones were highly cytotoxic at nanomolar doses against U87 and T98 cells. The therapeutic indexes (TI = IC50MRC5/IC50glioma) were 2-660 for T98 cells and 28-5000 for U87 cells, indicating that the studied hydrazones could be good antitumor drug candidates to treat brain tumors.

Published
2011

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