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

Biochemical and Biophysical Research Communications
Gabriela M AlmeidaFabiana Ourique

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)-2-phenylimidazo[1,2-a]pyridine, named IP-Se-05, and 3-((2-methoxyphenyl)selanyl)-7-methyl-2-phenylimidazo[1,2-a]pyridine, named IP-Se-06, showed high cytotoxicity for MCF-7 cells (IC50 = 26.0 μM and 12.5 μM, 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-a]pyridine (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.

Citations

Oct 24, 2020·Oxidative Medicine and Cellular Longevity·Tiago E A FrizonJamal Rafique
Mar 4, 2021·Chemical Record : an Official Publication of the Chemical Society of Japan ... [et Al.]·Jamal RafiqueAntonio L Braga
Aug 20, 2019·Bioorganic & Medicinal Chemistry Letters·Surendar ChittiKondapalli Venkata Gowri Chandra Sekhar
Jun 8, 2021·Angewandte Chemie·Marcelo Straesser FrancoAntonio Luiz Braga
Aug 8, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Giancarlo V BotteselleAntonio L Braga
Oct 1, 2021·Dalton Transactions : an International Journal of Inorganic Chemistry·Aditya UpadhyaySangit Kumar
Nov 16, 2021·Journal of Biomolecular Structure & Dynamics·Samima KhatunFirdoos Ahmad Sofi

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