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Type: Artigo
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
Subject: Atividade antitumoral
Country: França
Editor: Elsevier
Rights: Fechado
Identifier DOI: 10.1016/j.ejmech.2015.09.036
Date Issue: 2015
Appears in Collections:IB - Artigos e Outros Documentos
CPQBA - Artigos e Outros Documentos
FCF - Artigos e Outros Documentos

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