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Synthesis of PJOV56, a new quinoxalinyl-hydrazone derivative able to induce autophagy and apoptosis in colorectal cancer cells, and related compounds

2019; Elsevier BV; Volume: 30; Issue: 2 Linguagem: Inglês

10.1016/j.bmcl.2019.126851

1464-3405

Sarah Sant’Anna Maranhão, Andréa Felinto Moura, Augusto César Aragão Oliveira, Daisy Jereissati Barbosa Lima, Francisco Washington Araújo Barros Nepomuceno, Carlos Roberto Koscky Paier, Alessandra C. Pinheiro, Thaís Cristina Mendonça Nogueira, M.V.N. De Souza, Cláudia Pessoa,

Synthesis and biological activity

Quinoxaline derivatives are reported as antineoplastic agents against a variety of human cancer cell lines, with some compounds being submitted to clinical trials. In this work, we report the synthesis, characterization and cytotoxicity potential of a new series of quinoxalinyl-hydrazones. The most cytotoxic compound was (E)-2-[2-(2-pyridin-2-ylmethylene)hydrazinyl]quinoxaline (PJOV56) that presented a time-dependent effect against HCT-116 cells. After 48 h of incubation, PJOV56 was able to induce autophagy and apoptosis of HCT-116 cells, mediated by upregulation of Beclin 1, upregulation of LC3A/B II and activation of caspase 7. Apoptosis was induced along with G0/G1 cell cycle arrest at the highest concentration of PJOV56 (6.0 µM). Thus, PJOV56 showed a dose-dependent mode of action related to induction of autophagy and apoptosis in HCT-116 cells.