Please use this identifier to cite or link to this item: http://repositorio.unicamp.br/jspui/handle/REPOSIP/243720
Type: Artigo de periódico
Title: Synthesis Of Thiophene-thiosemicarbazone Derivatives And Evaluation Of Their In Vitro And In Vivo Antitumor Activities
Author: de Oliveira
Jamerson Ferreira; da Silva
Anekecia Lauro; Vendramini-Costa
Debora Barbosa; da Cruz Amorim
Cezar Augusto; Campos
Julia Furtado; Ribeiro
Amelia Galdino; de Moura
Ricardo Olimpio; Neves
Jorge Luiz; Tasca Gois Ruiz
Ana Lucia; de Carvalho
Joao Ernesto; Alves de Lima
Maria do Carmo
Abstract: A series of thiophene-2-thiosemicarbazones derivatives (5-14) was synthesized, characterized and evaluated for their antitumor activity. They were tested in vitro against human tumor cell lines through the colorimetric method. The results revealed that compounds 7 and 9 were the most effective in inhibiting 50% of the cell growth after 48 h of treatment. As compound 7 showed a potent anti-proliferative profile, it has been chosen for further studies in 786-0 cell line by flow cytometry. Treatments with compound 7 (50 mu M) induced early phosphatidylserine exposure after 18 h of exposure and this process progressed phosphatidylserine exposure with loss of cell membrane integrity after 24 h of treatment, suggesting a time-dependent cell death process. Regarding the cell cycle profile, no changes were observed after treatment with compound 7 (25 mu m), suggesting a mechanism of cell death independent on the cell cycle. The in vivo studies show that compound 7 possess low acute toxicity, being the doses of 30-300 mgK(-1) chosen for studies in Ehrlich solid tumor model in mice. All doses were able to inhibit tumor development being the lowest one the most effective. Our findings highlight thiophene-2-thiosemicarbazones as a promising class of compounds for further studies concerning new anticancer therapies. (C) 2015 Elsevier Masson SAS. All rights reserved.
Subject: Anticancer Drug Screen
Colorectal-cancer
Ribonucleotide Reductase
Multidrug-resistance
Kappa-b
Tumor
Agents
5-fluorouracil
Mechanisms
Inhibitor
Country: PARIS
Editor: ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
Citation: Synthesis Of Thiophene-thiosemicarbazone Derivatives And Evaluation Of Their In Vitro And In Vivo Antitumor Activities. Elsevier France-editions Scientifiques Medicales Elsevier, v. 104, p. 148-156 Nov-2015.
Rights: embargo
Identifier DOI: 10.1016/j.ejmech.2015.09.036
Address: http://www.sciencedirect.com/science/article/pii/S0223523415302804
Date Issue: 2015
Appears in Collections:Unicamp - Artigos e Outros Documentos

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