Document Type: Research article
Instituto Politecnico Nacional
Department of Chemistry, Quaid-i-Azam University, Islamabad, Pakistan
Centro de Nanociencias y Micro y Nanotecnología, Instituto Politécnico Nacional, México, D.F. México
Departamento de Química Aplicada, Universidad Autónoma de Tamaulipas, Reynosa, México
Neglected Diseases Section, Drug R&D Unit, Center for Applied Pharmacobiology Research, University of Navarra, Pamplona, España
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.