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(Referência obtida automaticamente do Web of Science, por meio da informação sobre o financiamento pela FAPESP e o número do processo correspondente, incluída na publicação pelos autores.)

Novel selenylated imidazo[1,2-a]pyridines for breast cancer chemotherapy: Inhibition of cell proliferation by Akt-mediated regulation, DNA cleavage and apoptosis

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Autor(es):
Almeida, Gabriela M. [1] ; Rafique, Jamal [2] ; Saba, Sumbal [2] ; Siminski, Tamila [1] ; Mota, Nadia S. R. S. [1] ; Wilhelm Filho, Danilo [3] ; Braga, Antonio Luiz [2] ; Pedrosa, Rozangela Curi [1] ; Ourique, Fabiana [1]
Número total de Autores: 9
Afiliação do(s) autor(es):
[1] Univ Fed Santa Catarina, Dept Bioquim, Lab Bioquim Expt LABIOEX, Florianopolis, SC - Brazil
[2] Univ Fed Santa Catarina, Dept Quim, Lab Sintese Subst Selenio Bioativas LabSelen, BR-88040900 Florianopolis, SC - Brazil
[3] Univ Fed Santa Catarina, Ecol & Zool Dept, Florianopolis, SC - Brazil
Número total de Afiliações: 3
Tipo de documento: Artigo Científico
Fonte: Biochemical and Biophysical Research Communications; v. 503, n. 3, p. 1291-1297, SEP 10 2018.
Citações Web of Science: 9
Resumo

A novel series of selenylated imidazo{[}1,2-a]pyridines were designed and synthesized with a view to a promising activity against breast cancer cell. The compounds, 7-methyl-3-(naphthalene-1-ylselanyl)-2phenylimidazo{[}1,2-a]pyridine, named IP-Se-05, and 34(2-methoxyphenyl)selany1)-7-methyl-2phenylimidazo{[}1,2-a]pyridine, named IP-Se-06, showed high cytotoxicity for MCF-7 cells (IC50= 26.0 mu M and 12.5 mu M, respectively). Both the compounds inhibited the cell proliferation and caused decrease in the number of cells in the G2/M phase of cell cycle. IP-Se-05 and IP-Se-06 were also evaluated for effects on CT DNA and DNA of MCF-7 cells. The compounds intercalated into CT-DNA and both treatments caused cleavage of DNA in cells. In addition, the compounds induced cell death by apoptosis. However, the presence of (2-methoxyphenyl) selenyl moiety at the imidazo{[}1,2-ajpyridine (IP-Se-06) appears to have a better antitumor effect with higher cytotoxicity at a lower concentration and caused less necrosis. Overall, the current study established IP-Se-06 more than IP-Se-05 as a potential prototype compound to be employed as an antiproliferative agent for the treatment of breast cancer. (C) 2018 Elsevier Inc. All rights reserved. (AU)

Processo FAPESP: 14/50249-8 - Green chemistry: sustainable synthetic methods employing benign solvents, safer reagents, and bio-renewable feedstock
Beneficiário:Arlene Gonçalves Corrêa
Modalidade de apoio: Auxílio à Pesquisa - Programa Centros de Pesquisa em Engenharia