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http://hdl.handle.net/1843/70458| Tipo: | Artigo de Periódico |
| Título: | Pharmacological and physicochemical profile of arylacetamides as tools against human cancers |
| Autor(es): | Paulo Michel Pinheiro Ferreira Kátia da Conceição Machado Stefânia Neiva Lavorato Fátima de Cássia Evangelista de Oliveira Jurandy do Nascimento Silva Antonia Amanda Cardoso de Almeida Luciano de Souza Santos Valdenizia Rodrigues Silva Daniel Pereira Bezerra Milena Botelho Pereira Soares Cláudia Pessoa Manoel Odorico de Moraes Filho José Roberto de Oliveira Ferreira João Marcelo de Castro e Sousa Vinícius Gonçalves Maltarollo Ricardo José Alves |
| Resumen: | Arylacetamides are widely used as synthetic intermediates to obtain medicinal substances. This work evaluated in vitro antiproliferative activity of ten 2-Chloro-N-arylacetamides on human normal and cancer cells and detailed in vivo toxicological and anticancer investigations. Initially, cytotoxic colorimetric assays were performed using tumor lines, peripheral blood mononuclear cells (PBMC) and erythrocytes. Compounds 2, 3 and 4 were tested for acute toxicity (50, 150 and 300mg/kg) and for subacute antitumoral capacity in HCT-116 colon carcinoma-bearing xenograft mice for 15days at 25mg/kg/day. Most compounds revealed cytotoxic action on tumor lines and PBMC, but activity on human erythrocytes were not detected. Molecular dipole moment, lipophilicity and electronic constant of aryl substituents had effects upon in vitro antiproliferative capacity. More common in vivo acute behavioral signals with compounds 2, 3 and 4 were muscle relaxation, reduction of spontaneous locomotor activity and number of entries in closed arms and increased number of falls andtime spent in open arms, suggesting diazepam-like anxiolytic properties. Decrease of grabbing strength and overall activity were common, but palpebral ptosis and deaths occurred at 300mg/kg only. Compounds 2 and 3 reduced colon carcinoma growth (21.2 and 27.5%, respectively, p < 0.05) without causing apparent signals of organspecific toxicity after subacute exposure. The structural chemical simplicity of arylacetamides make them costeffective alternatives and justifies further improvements to enhance activity, selectivity and the development of pharmaceutical formulations. |
| Asunto: | Neoplasias do Colo Ensaios antitumorais modelo de xenoenxerto |
| Idioma: | eng |
| País: | Brasil |
| Editor: | Universidade Federal de Minas Gerais |
| Sigla da Institución: | UFMG |
| Departamento: | FAR - DEPARTAMENTO DE PRODUTOS FARMACÊUTICOS |
| Tipo de acceso: | Acesso Aberto |
| Identificador DOI: | 10.1016/j.taap.2019.114692 |
| URI: | http://hdl.handle.net/1843/70458 |
| Fecha del documento: | oct-2019 |
| metadata.dc.url.externa: | https://www.sciencedirect.com/science/article/pii/S0041008X1930300X |
| metadata.dc.relation.ispartof: | Toxicology and Applied Pharmacology |
| Aparece en las colecciones: | Artigo de Periódico |
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| archivo | Descripción | Tamaño | Formato | |
|---|---|---|---|---|
| Pharmacological and physicochemical profile of arylacetamides as tools against human cancers.pdf | 892.33 kB | Adobe PDF | Visualizar/Abrir |
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