| Full text | |
| Author(s): |
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]
Total Authors: 9
|
| Affiliation: | [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
Total Affiliations: 3
|
| Document type: | Journal article |
| Source: | Biochemical and Biophysical Research Communications; v. 503, n. 3, p. 1291-1297, SEP 10 2018. |
| Web of Science Citations: | 9 |
| Abstract | |
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) | |
| FAPESP's process: | 14/50249-8 - Green chemistry: sustainable synthetic methods employing benign solvents, safer reagents, and bio-renewable feedstock |
| Grantee: | Arlene Gonçalves Corrêa |
| Support Opportunities: | Research Grants - Research Centers in Engineering Program |