Pharmacological and physicochemical profile of arylacetamides as tools against human cancers

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dc.creatorPaulo Michel Pinheiro Ferreira
dc.creatorKátia da Conceição Machado
dc.creatorStefânia Neiva Lavorato
dc.creatorFátima de Cássia Evangelista de Oliveira
dc.creatorJurandy do Nascimento Silva
dc.creatorAntonia Amanda Cardoso de Almeida
dc.creatorLuciano de Souza Santos
dc.creatorValdenizia Rodrigues Silva
dc.creatorDaniel Pereira Bezerra
dc.creatorMilena Botelho Pereira Soares
dc.creatorCláudia Pessoa
dc.creatorManoel Odorico de Moraes Filho
dc.creatorJosé Roberto de Oliveira Ferreira
dc.creatorJoão Marcelo de Castro e Sousa
dc.creatorVinícius Gonçalves Maltarollo
dc.creatorRicardo José Alves
dc.date.accessioned2024-07-12T18:31:25Z
dc.date.accessioned2025-09-09T00:06:36Z
dc.date.available2024-07-12T18:31:25Z
dc.date.issued2019-10
dc.format.mimetypepdf
dc.identifier.doi10.1016/j.taap.2019.114692
dc.identifier.issn0041008X
dc.identifier.urihttps://hdl.handle.net/1843/70458
dc.languageeng
dc.publisherUniversidade Federal de Minas Gerais
dc.relation.ispartofToxicology and Applied Pharmacology
dc.rightsAcesso Aberto
dc.subjectNeoplasias do Colo
dc.subjectEnsaios antitumorais modelo de xenoenxerto
dc.subject.otherColon carcinoma
dc.subject.otherXenograft model
dc.subject.otherPhysiological parameters
dc.subject.otherAnxiolytic-like effects
dc.subject.otherBehavioral animal
dc.titlePharmacological and physicochemical profile of arylacetamides as tools against human cancers
dc.typeArtigo de periódico
local.citation.epage114702
local.citation.spage114692
local.citation.volume380
local.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.
local.publisher.countryBrasil
local.publisher.departmentFAR - DEPARTAMENTO DE PRODUTOS FARMACÊUTICOS
local.publisher.initialsUFMG
local.url.externahttps://www.sciencedirect.com/science/article/pii/S0041008X1930300X

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