Quinoxaline-1,4-dioxide derivatives inhibitory action in melanoma and brain tumor cells

Future Med Chem. 2019 Apr;11(7):645-657. doi: 10.4155/fmc-2018-0251. Epub 2019 Apr 9.

Abstract

Aim: Quinoxaline-1,4-dioxide derivatives are synthetic heterocyclic compounds with multiple biological and pharmacological effects. In this study, we investigated the bioactivity of five quinoxaline-1,4-di-N-oxides derivatives in different animal cell lines. Materials & methods: Using in vitro cell cultures, we evaluated the influence of quinoxaline-1,4-dioxide, 2-methylquinoxaline-1,4-dioxide, 2-amino-3-cyanoquinoxaline-1,4-dioxide, 3-methyl-2-quinoxalinecarboxamide-1,4-dioxide and 2-hydroxyphenazine-N,N-dioxide (2HF) in the viability, migration and proliferation of nonmalignant (3T3-L1 and human dermal microvascular endothelial cell) and malignant (B16-F10, MeWo, GL-261 and BC3H1) cell lines. Results: The viability IC50 concentrations for each quinoxaline-1,4-di-N-oxide derivative were calculated, and a concomitant reduction of migration and proliferation was observed mainly in malignant cell lines. Conclusion: 2HF exhibited potent anti-viability, anti-migration and anti-proliferative actions selectively in tumor cells, nevertheless more studies are required to further investigate 2HF promising biologic effects.

Keywords: 1,4-benzodiazine derivatives; anticancer; bioactivity; brain tumor; melanoma.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology
  • Brain Neoplasms / drug therapy*
  • Cell Line, Tumor
  • Cell Movement
  • Cell Proliferation
  • Cell Survival
  • Drug Screening Assays, Antitumor / methods
  • Humans
  • Melanoma / drug therapy*
  • Mice
  • Molecular Structure
  • Quinoxalines / chemistry*
  • Quinoxalines / pharmacology
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Quinoxalines
  • quindoxin