Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 6 de 6
Filtrar
Mais filtros










Base de dados
Intervalo de ano de publicação
1.
RSC Adv ; 13(26): 17812-17816, 2023 Jun 09.
Artigo em Inglês | MEDLINE | ID: mdl-37323449

RESUMO

A class of indenopyrroles is presented by the treatment of known dihydroxy-2-methyl-4-oxoindeno[1,2-b]pyrroles with phosphorus oxychloride (POCl3). The elimination of vicinal hydroxyl groups at the 3a and 8b positions, formation of a π bond, and electrophilic chlorination of the methyl group attached to C2 resulted in the fused aromatic pyrrole structures. Benzylic substitution of various nucleophiles such as H2O, EtOH, and NaN3 with a chlorine atom gave diverse 4-oxoindeno[1,2-b]pyrrole derivatives in 58 to 93% yields. The reaction was investigated in different aprotic solvents, and the highest reaction yield was obtained in DMF. The structures of the products were confirmed by spectroscopic methods, elemental analysis, and X-ray crystallography.

2.
RSC Adv ; 11(58): 36958-36964, 2021 Nov 10.
Artigo em Inglês | MEDLINE | ID: mdl-35494384

RESUMO

Four polysaccharides (chitosan, cellulose, starch, and pectin) were magnetized with magnetic iron oxide (Fe3O4) and then sulfonated (except pectin) with chlorosulfonic acid. The obtained solid acids were used as a catalyst in three-component reactions between N-substituted-2-formylpyrrole, hydroxylamine-hydrochloride, and ß-keto esters for the synthesis of 4-(2-pyrrolyl) methylene-isoxazole-5-ones. The optimal catalyst system was selected and studied by IR, SEM, TEM and XRD methods. The diverse isoxazoline derivatives (obtained via a mild and simple approach) were also fully characterized by spectroscopic methods and screened for anti-cancer activities against HT-29 and MCF-7 colon and breast cancer and HEK 293 normal cells. The results revealed interesting anti-cancer activities.

3.
J Biol Inorg Chem ; 25(3): 411-417, 2020 05.
Artigo em Inglês | MEDLINE | ID: mdl-32146511

RESUMO

The aim of the present study was to evaluate the H2O2 scavenging activity of the ZnO2/ß-CD as a biocompatible composite. Zinc peroxide was prepared via sonochemical approach. To synthesize a green composite, ß-cyclodextrin was modified by citric acid (CA) and reacted with ZnO2 under ultrasonic irradiation. The prepared samples were characterized using XRD, SEM, TGA and FTIR analytical techniques. XRD analysis exhibited a typical pattern of ZnO2 and demonstrated the presence of citric acid and ß-cyclodextrin in composite. The results of the catalytic assay showed that the ZnO2/CA-ßCD composite displayed stronger capability to decompose H2O2 in comparison to ZnO2 particles (about seven times). It was attributed to increased adsorption capacity and solubility of composite due to the presence of citric acid and ß-cyclodextrin. MTT assay studies confirmed the non-cytotoxic nature of ZnO2 particles and ZnO2/CA-ßCD composite.


Assuntos
Materiais Biocompatíveis/química , Ácido Cítrico/química , Sequestradores de Radicais Livres/química , Peróxido de Hidrogênio/química , Óxido de Zinco/química , beta-Ciclodextrinas/química , Adsorção , Células Cultivadas , Humanos , Estrutura Molecular , Tamanho da Partícula , Solubilidade , Propriedades de Superfície , Ondas Ultrassônicas , Óxido de Zinco/síntese química
4.
Carbohydr Polym ; 226: 115310, 2019 Dec 15.
Artigo em Inglês | MEDLINE | ID: mdl-31582060

RESUMO

This study reports the synthesis and characterization of a highly active catalyst based on chelated copper iodide on magnetic chitosan-salicylaldehyde Schiff base. This catalyst was successfully used for the three-component reaction of N-propargylphthalimide, tosylazide, and NH or OH containing nucleophiles to access new classes of N-sulfonylamidine or N-sulfonylimidate derivatives. The products, which were constructed via an in situ generated sulfonyl keteneimine intermediate, were obtained in good to excellent yields. Short reaction times, easy separation and reusability without significant loss of catalyst activity were found to be the notable features of this synthetic protocol.

5.
Artigo em Inglês | MEDLINE | ID: mdl-30931800

RESUMO

Stilbene derivatives have been found to possess promising anticancer activities against human cancer cell lines in vitro. In the present study, we have investigated cytotoxic, apoptosis induction and DNA binding activity of new stilbene derivative, (E)-1-(4-Chlorophenyl)-4,5-diphenyl-2-[4-(4-methoxystryl)phenyl]-1H-imidazol (STIM) on K562 chronic myeloid leukemia cell line. Via MTT assay STIM demonstrated cytotoxic activity against K562 cell line with IC50 value of 150 µM. Apoptosis, as the mechanism of cell death, was evaluated by morphological study and flow cytometric analysis. In vitro DNA binding property of STIM has been studied by vital spectroscopic techniques, which indicated that STIM interact with ctDNA through groove binding mode and binding constant (Kb) was estimated to be 6.9 × 104 M-1. Docking studies revealed that hydrophobic is the most important interaction in STIM-DNA complex, and that the ligand (STIM) interacts with DNA via groove binding mode and the bindiyspng energy was calculated as -13.37 kcal/mol. Taken together, the present study suggests that STIM exhibits anticancer effect on K562 cell line through the induction of apoptosis as well as cell cycle arrest at Sub-G1 phase and also can bind to double helix DNA in vitro.


Assuntos
Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , DNA/efeitos dos fármacos , Simulação de Acoplamento Molecular , Estilbenos/farmacologia , Animais , Antineoplásicos/síntese química , Antineoplásicos/química , Sítios de Ligação/efeitos dos fármacos , Bovinos , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Células K562 , Estrutura Molecular , Estilbenos/síntese química , Estilbenos/química , Relação Estrutura-Atividade , Células Tumorais Cultivadas
6.
Pharm Res ; 36(5): 68, 2019 Mar 18.
Artigo em Inglês | MEDLINE | ID: mdl-30887127

RESUMO

PURPOSE: Chemotherapy as an important tool for cancer treatment faces many obstacles such as multidrug resistance and adverse toxic effects on healthy tissues. Drug delivery systems have opened a new window to overcome these problems. METHODS: A polyelectrolyte carboxymethyl cellulose polymer as a magnetic nanocarrier was synthesized for enhancing delivery and uptake of doxorubicin in MCF7 breast cancer cells and decreasing the adverse toxic effects to healthy tissues. RESULTS: The physicochemical properties of developed nanocarrier showed that it can be used in drug delivery purposes. The efficiency of the delivery system was assessed by loading and release studies. Besides, biological assays including protein-particle interaction, hemolysis assay, cytotoxicity study, cellular uptake, and apoptosis analysis were performed. All results persuaded us to investigate the cytotoxic effects of nanocarrier in an animal model by determining the biochemical parameters attributed to organ injuries, and hematoxylin and eosin (H&E) staining for histopathological manifestations. We observed that the nanocarrier has no toxic effect on healthy tissues, while, it is capable of reducing the toxic side effects of doxorubicin by more cellular internalization. CONCLUSION: Chemical characterizations and biological studies confirmed that developed nanocarrier with permanent cationic groups of imidazolium and anionic carboxylic acid groups is an effective candidate for anticancer drug delivery.


Assuntos
Antineoplásicos/administração & dosagem , Carboximetilcelulose Sódica/química , Doxorrubicina/administração & dosagem , Portadores de Fármacos/química , Polieletrólitos/química , Animais , Antineoplásicos/toxicidade , Apoptose/efeitos dos fármacos , Carboximetilcelulose Sódica/toxicidade , Permeabilidade da Membrana Celular , Sobrevivência Celular/efeitos dos fármacos , Doxorrubicina/toxicidade , Portadores de Fármacos/toxicidade , Liberação Controlada de Fármacos , Humanos , Células MCF-7 , Nanopartículas de Magnetita/química , Masculino , Camundongos , Tamanho da Partícula , Polieletrólitos/toxicidade , Propriedades de Superfície
SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA
...