Please use this identifier to cite or link to this item: http://repositorio.unicamp.br/jspui/handle/REPOSIP/235363
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, Anekécia Lauro
Vendramini-Costa, Débora Barbosa
da Cruz Amorim, Cezar Augusto
Campos, Júlia Furtado
Ribeiro, Amélia Galdino
Olímpio de Moura, Ricardo
Neves, Jorge Luiz
Ruiz, Ana Lúcia Tasca Gois
Ernesto de Carvalho, João
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 antiproliferative profile, it has been chosen for further studies in 786-0 cell line by flow cytometry. Treatments with compound 7 (50 μM) 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 μM), 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 mgKg(-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: Antitumor
Cytotoxicity
Medicinal Chemistry
Thiophene
Thiosemicarbazone
Rights: embargo
Identifier DOI: 10.1016/j.ejmech.2015.09.036
Address: http://www.ncbi.nlm.nih.gov/pubmed/26454648
Date Issue: 2015
Appears in Collections:Unicamp - Artigos e Outros Documentos

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