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Please use this identifier to cite or link to this item: http://hdl.handle.net/1843/70458
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dc.creatorPaulo Michel Pinheiro Ferreirapt_BR
dc.creatorKátia da Conceição Machadopt_BR
dc.creatorStefânia Neiva Lavoratopt_BR
dc.creatorFátima de Cássia Evangelista de Oliveirapt_BR
dc.creatorJurandy do Nascimento Silvapt_BR
dc.creatorAntonia Amanda Cardoso de Almeidapt_BR
dc.creatorLuciano de Souza Santospt_BR
dc.creatorValdenizia Rodrigues Silvapt_BR
dc.creatorDaniel Pereira Bezerrapt_BR
dc.creatorMilena Botelho Pereira Soarespt_BR
dc.creatorCláudia Pessoapt_BR
dc.creatorManoel Odorico de Moraes Filhopt_BR
dc.creatorJosé Roberto de Oliveira Ferreirapt_BR
dc.creatorJoão Marcelo de Castro e Sousapt_BR
dc.creatorVinícius Gonçalves Maltarollopt_BR
dc.creatorRicardo José Alvespt_BR
dc.date.accessioned2024-07-12T18:31:25Z-
dc.date.available2024-07-12T18:31:25Z-
dc.date.issued2019-10-
dc.citation.volume380pt_BR
dc.citation.spage114692pt_BR
dc.citation.epage114702pt_BR
dc.identifier.doi10.1016/j.taap.2019.114692pt_BR
dc.identifier.issn0041008Xpt_BR
dc.identifier.urihttp://hdl.handle.net/1843/70458-
dc.description.resumoArylacetamides 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.pt_BR
dc.format.mimetypepdfpt_BR
dc.languageengpt_BR
dc.publisherUniversidade Federal de Minas Geraispt_BR
dc.publisher.countryBrasilpt_BR
dc.publisher.departmentFAR - DEPARTAMENTO DE PRODUTOS FARMACÊUTICOSpt_BR
dc.publisher.initialsUFMGpt_BR
dc.relation.ispartofToxicology and Applied Pharmacology-
dc.rightsAcesso Abertopt_BR
dc.subjectColon carcinomapt_BR
dc.subjectXenograft modelpt_BR
dc.subjectPhysiological parameterspt_BR
dc.subjectAnxiolytic-like effectspt_BR
dc.subjectBehavioral animalpt_BR
dc.subject.otherNeoplasias do Colopt_BR
dc.subject.otherEnsaios antitumorais modelo de xenoenxertopt_BR
dc.titlePharmacological and physicochemical profile of arylacetamides as tools against human cancerspt_BR
dc.typeArtigo de Periódicopt_BR
dc.url.externahttps://www.sciencedirect.com/science/article/pii/S0041008X1930300Xpt_BR
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