[:pb]Authors: Maranhão, S.S.; Moura, A. F.; Oliveira, A. C. A.; Lima, D. J. B.; Barros-Nepomuceno, F. W. A.; Paier, C. R. K.; Pinheiro, A. C.; Nogueira, T. C. M.; De Souza, M. V. N.; Pessoa, C.
Source: Bioorganic & Medicinal Chemistry Letters, v. 30, p. 126851-126851, 2020.
Publisher: ScienceDirect
Abstract
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.
Keywords: quinoxalines, cytotoxicity, HCT-116 cells, cell cycle arrest
Document Type: Research Article
DOI: 10.1016/j.bmcl.2019.126851
Publication date: 15 de Janeiro de 2020[:]
