| Author | Ferreira, Paulo Michel Pinheiro | |
| Author | Machado, Kátia da Conceição | |
| Author | Lavorato, Stefânia Neiva | |
| Author | Oliveira, Fátima de Cássia Evangelista de | |
| Author | Silva, Jurandy do Nascimento | |
| Author | Almeida, Antonia Amanda Cardoso de | |
| Author | Santos, Luciano de Souza | |
| Author | Silva, Valdenizia Rodrigues | |
| Author | Bezerra, Daniel Pereira | |
| Author | Soares, Milena Botelho Pereira | |
| Author | Pessoa, Cláudia | |
| Author | Moraes Filho, Manoel Odorico de | |
| Author | Ferreira, José Roberto de Oliveira | |
| Author | Sousa, João Marcelo de Castro E | |
| Author | Maltarollo, Vinícius Gonçalves | |
| Author | Alves, Ricardo José | |
| Access date | 2019-10-01T18:02:45Z | |
| Available date | 2019-10-01T18:02:45Z | |
| Document date | 2019 | |
| Citation | FERREIRA, Paulo Michel Pinheiro et al. Pharmacological and physicochemical profile of arylacetamides as tools against human cancers. Toxicology and Applied Pharmacology, v. 380, p. 1-11, 2019. | pt_BR |
| ISSN | 0041-008X | pt_BR |
| URI | https://www.arca.fiocruz.br/handle/icict/36051 | |
| Sponsorship | “Coordenação de Aperfeiçoamento de Pessoal de Nível Superior” –
Brasil (CAPES) – Finance code 001. This study was financed in part by
the Brazilian agency “Coordenação de Aperfeiçoamento de Pessoal de
Nível Superior” – Brasil (CAPES) – Finance code 001. Dr. Paulo Michel
Pinheiro Ferreira is grateful to the Conselho Nacional de
Desenvolvimento Científico e Tecnológico” [CNPq (#305086/2016-2)]
for the personal scholarship. | pt_BR |
| Language | eng | pt_BR |
| Publisher | Elsevier | pt_BR |
| Rights | restricted access | pt_BR |
| Subject in Portuguese | Carcinoma de Cólon | pt_BR |
| Subject in Portuguese | Modelo Xenoenxerto | pt_BR |
| Subject in Portuguese | Parâmetros Fisiológicos | pt_BR |
| Subject in Portuguese | Efeitos Ansiolíticos | pt_BR |
| Subject in Portuguese | Animal Comportamental | pt_BR |
| Title | Pharmacological and physicochemical profile of arylacetamides as tools against human cancers | pt_BR |
| Type | Article | |
| DOI | 10.1016/j.taap.2019.114692 | |
| Abstract | 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 300 mg/kg) and for subacute antitumoral capacity in HCT-116 colon carcinoma-bearing xenograft mice for 15 days at 25 mg/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 300 mg/kg only. Compounds 2 and 3 reduced colon carcinoma growth (21.2 and 27.5%, respectively, p < 0.05) without causing apparent signals of organ-specific toxicity after subacute exposure. The structural chemical simplicity of arylacetamides make them cost-effective alternatives and justifies further improvements to enhance activity, selectivity and the development of pharmaceutical formulations. | pt_BR |
| Affilliation | Federal University of Piauí. Laboratory of Experimental Cancerology. Department of Biophysics and Physiology. Teresina, PI, Brazil / Federal University of Piauí. Postgraduate Programs in Pharmaceutical Sciences and Biotechnology. Teresina, PI, Brazil. | pt_BR |
| Affilliation | Federal University of Piauí. Laboratory of Experimental Cancerology. Department of Biophysics and Physiology. Teresina, PI, Brazil / Federal University of Piauí. Postgraduate Programs in Pharmaceutical Sciences and Biotechnology. Teresina, PI, Brazil. | pt_BR |
| Affilliation | Federal University of Minas Gerais. Faculty of Pharmacy. Department of Pharmaceutical Products. Belo Horizonte, MG, Brazil / Federal University of Western Bahia. Center of Biological Sciences and Health. Barreiras, BA, Brazil. | pt_BR |
| Affilliation | Federal University of Ceará. Faculty of Medicine. Department of Physiology and Pharmacology. Fortaleza, CE, Brazil. | pt_BR |
| Affilliation | Federal University of Piauí. Laboratory of Experimental Cancerology. Department of Biophysics and Physiology. Teresina, PI, Brazil / Federal University of Piauí. Postgraduate Programs in Pharmaceutical Sciences and Biotechnology. Teresina, PI, Brazil. | pt_BR |
| Affilliation | Federal University of Piauí. Laboratory of Experimental Cancerology. Department of Biophysics and Physiology. Teresina, PI, Brazil / Federal University of Piauí. Postgraduate Programs in Pharmaceutical Sciences and Biotechnology. Teresina, PI, Brazil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Gonçalo Moniz. Salvador, BA, Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Gonçalo Moniz. Salvador, BA, Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Gonçalo Moniz. Salvador, BA, Brasil. | pt_BR |
| Affilliation | Federal University of Ceará. Faculty of Medicine. Department of Physiology and Pharmacology. Fortaleza, CE, Brazil. | pt_BR |
| Affilliation | Federal University of Ceará. Faculty of Medicine. Department of Physiology and Pharmacology. Fortaleza, CE, Brazil. | pt_BR |
| Affilliation | State University of Alagoas. School of Medical Sciences. Maceió, AL, Brazil. | pt_BR |
| Affilliation | Federal University of Piauí. Postgraduate Programs in Pharmaceutical Sciences and Biotechnology. Teresina, PI, Brazil / Federal University of Piauí. Department of Biology. Picos, PI, Brazil. | pt_BR |
| Affilliation | Federal University of Minas Gerais. Faculty of Pharmacy. Department of Pharmaceutical Products. Belo Horizonte, MG, Brazil. | pt_BR |
| Affilliation | Federal University of Minas Gerais. Faculty of Pharmacy. Department of Pharmaceutical Products. Belo Horizonte, MG, Brazil. | pt_BR |
| Subject | Colon Carcinoma | pt_BR |
| Subject | Xenograft Model | pt_BR |
| Subject | Physiological Parameters | pt_BR |
| Subject | Anxiolytic-like Effects | pt_BR |
| Subject | Behavioral Animal | pt_BR |
