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Synthesis and evaluation of platinum complexes with potential antitumor activity BJPS
Freire,Rachel Lima Marcelino; Marques,Maria Betânia de Freitas; Souza-Fagundes,Elaine Maria de; Oliveira,Renata Barbosa de; Alves,Ricardo José.
Abstract A novel series of platinum (II) complexes was synthesized and the complexes were evaluated for their in vitro cytotoxicity against four human cancer cells lines. Five platinum complexes showed activity against at least one tumor cell line. Complexes 3 and 6 were promising, being active, at micromolar concentrations, against all the assayed tumor cell lines. Compound 3 was selected for further studies in mice with Ehrlich solid tumors and it was able to reduce the rate of tumor growth significantly during the first seven days. However, at the end of the experiments, there was no significant difference between the group of animals treated with 3 and the control group. The low solubility of the compound in the assay conditions can explain, at least...
Tipo: Info:eu-repo/semantics/article Palavras-chave: /Cytotoxic activity; Platinum complexes/ Ehrlich solid tumor activity..
Ano: 2017 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502017000100612
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Assessment of anti-diabetic activity of a novel hydrazine-thiazole derivative: in vitro and in vivo method BJPS
Resende,Marina Ferrara de; Lino,Cleudiomar Inácio; Souza-Fagundes,Elaine Maria de; Rettore,João Vitor Paes; Oliveira,Renata Barbosa de; Labanca,Renata Adriana.
Diabetes mellitus is a chronic disease resulting in oxidative stress that promotes tissue damage. The appearance of this disease is highly related to lifestyle and food of the population, being of great interest to search for a dietary supplement that can also act by reducing oxidative alterations. Based on the broad range of biological activity of thiazole derivatives, this work aimed to evaluate the in vitro antioxidant activity of a novel hydrazine-thiazole derivative and studies in vivo. In in vivo experiments, the liver extracts of healthy and diabetic Wistar rats were used, with analysis to determine the enzymatic activity of SOD, CAT, GPx, and GR, and determination of lipid peroxidation. Finally, in the blood of these animals, biochemical parameters...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Oxidative stress; Diabetes mellitus; Curcumin; Thiazole derivatives; Dietary supplement.
Ano: 2019 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502019000100509
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Oxcarbazepine: validation and application of an analytical method BJPS
Enéas,Paula Cristina Rezende; Oliveira,Renata Barbosa de; Pianetti,Gerson Antônio.
Oxcarbazepine (OXC) is an important anticonvulsant and mood stabilizing drug. A pharmacopoeial monograph for OXC is not yet available and therefore the development and validation of a new analytical method for quantification of this drug is essential. In the present study, a UV spectrophotometric method for the determination of OXC was developed. The various parameters, such as linearity, precision, accuracy and specificity, were studied according to International Conference on Harmonization Guidelines. Batches of 150 mg OXC capsules were prepared and analyzed using the validated UV method. The formulations were also evaluated for parameters including drug-excipient compatibility, flowability, uniformity of weight, disintegration time, assay, uniformity of...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Oxcarbazepine/quantitative analysis; Anticonvulsants/quantitative analysis; UV spectrophotometric/method validation; Capsules/dissolution.
Ano: 2010 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502010000200013
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Synthesis and cytotoxicity evaluation of thiosemicarbazones and their thiazole derivatives BJPS
Braga,Saulo Feheiberg Pinto; Fonseca,Nayara Cristina; Ramos,Jonas Pereira; Souza-Fagundes,Elaine Maria de; Oliveira,Renata Barbosa de.
ABSTRACT The aims of this study were to synthesize a series of thiosemicarbazones and their thiazole derivatives, to investigate their cytotoxic activity against three human cancers and normal (Vero cells) cell lines, and to evaluate the pro-apoptotic potential of the most active compounds. Materials and Methods: The thiosemicarbazones were obtained by reacting an aromatic aldehyde with thiosemicarbazide (yield 71-96%), which were subjected to a cyclization with α-bromoacetophenone to yield the required thiazole heterocycles (yield 63-100%). All the synthesized compounds were screened at 50 µM concentration against three cell lines representing HL60 (promyelocytic leukemia), Jurkat (acute lymphoblastic leukemia), and MCF-7 (breast cancer). The...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Thiosemicarbazones/synthesis; Thiosemicarbazones/cytotoxic activity; Thiazoles/derivatives/synthesis; Thiazoles/derivatives/cytotoxic activity.
Ano: 2016 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502016000200299
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Ortho-nitrobenzyl derivatives as potential anti-schistosomal agents BJPS
Lopes,Marcela Silva; Suzuki,Brian Michio; Pereira,Glaécia Aparecida do Nascimento; Probst,Alexandra Christina; Ferreira,Rafaela Salgado; Oliveira,Júlia Teixeira de; Tecchio,Kimberly Brito; Santos,Fabio Vieira dos; Caffrey,Conor Robert; Oliveira,Renata Barbosa de.
ABSTRACT In the search for new anti-schistosomal agents, a series of fifteen ortho-nitrobenzyl derivatives was assayed in vitro against both the schistosomulum (somule) and adult forms of Schistosoma mansoni. Compounds 8 and 12 showed significant activity against somules at low micromolar concentrations, but none was active against adults. The SAR demonstrated that the compounds most active against the parasite were mutagenic to the human cell line RKO-AS45-1 only at concentrations 10- to 40-fold higher than the worm-killing dose. Given their electrophilicity, compounds were also screened as inhibitors of the S. mansoni cysteine protease (cathepsin B1) in vitro. Amides 5 and 15 exhibited a modest inhibition activity with values of 55.7 and 50.6 % at 100...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Nitro-aromatic; Schistosoma mansoni/ anti-schistosomal activity; Cathepsin B1; Mutagenicity.
Ano: 2018 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502018000200613
Registros recuperados: 5
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