Esters of Quinoxaline 1,4-di-N-oxide with Cytotoxic Activity on Tumor Cell Lines Based on NCI-60 Panel

Document Type: Research article


1 Instituto Politecnico Nacional

2 Department of Chemistry, Quaid-i-Azam University, Islamabad, Pakistan

3 Centro de Nanociencias y Micro y Nanotecnología, Instituto Politécnico Nacional, México, D.F. México

4 Departamento de Química Aplicada, Universidad Autónoma de Tamaulipas, Reynosa, México

5 Neglected Diseases Section, Drug R&D Unit, Center for Applied Pharmacobiology Research, University of Navarra, Pamplona, España

6 Departamento de Inmunología, Escuela Nacional de Ciencias Biológicas, México D.F., México.


Quinoxalines display diverse and interesting pharmacological activities as antibacterial, antiviral, antiparasitic and anticancer agents. Particularly, their 1,4-di-N-oxides derivatives have proved to be cytotoxic agents that are active under hypoxic conditions as that of solid tumours. A new series of quinoxaline 1,4-di-N-oxides substitutes at 7-position with esters group were synthetized and characterized by infrared (IR), proton nuclear magnetic resonance (1H-NMR) spectroscopy, and elemental analysis. Seventeen derivatives (M1-M3, E1-E8, P1-P3 and DR1-DR3) were selected and evaluated for antitumor activities using the NCI-60 human tumor cell lines screen. Results showed that E7, P3 and E6 were the most active compounds against the cell lines tested. Substitutions at 7-position with esters group not necessarily affect the biological activity, but the nature of the esters group could exert an influence on the selectivity. Additionally, substitutions at 2-position influenced the cytotoxic activity of the compounds.


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