Author/Authors :
Rivera, Gildardo Centro de Biotecnología Genómica - Instituto Politécnico Nacional, Reynosa, México , Ahmad Shah, Shoaib Department of Chemistry - Quaid-i-Azam University, Islamabad, Pakistan , Arrieta-Baez, Daniel Centro de Nanociencias y Micro y Nanotecnología - Instituto Politécnico Nacional, Ciudad de México, México , Palos, Isidro Departamento de Química Aplicada - Universidad Autónoma de Tamaulipas, Reynosa, México , Mongue, Antonio Neglected Diseases Section - Drug R& D Unit - Center for Applied Pharmacobiology Research - University of Navarra, Pamplona, Espana , Enid Sánchez-Torres, Luvia Departamento de Inmunología - Escuela Nacional de Ciencias Biológicas - Instituto Politécnico Nacional, Ciudad de México, México
Abstract :
Quinoxalines display diverse and interesting pharmacological activities as antibacterial,
antiviral, antiparasitic and anticancer agents. Particularly, their 1ˏ4-di-N-oxide derivatives have
proved to be cytotoxic agents that are active under hypoxic conditions as that of solid tumours.
A new series of quinoxaline 1ˏ4-di-N-oxide 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.
Keywords :
Quinoxaline 1, 4-di-N-oxide , Esters , Drugs , Cancer , Antitumor
