Title of article
Esters of Quinoxaline 1ˏ4-Di-N-oxide with Cytotoxic Activity on Tumor Cell Lines Based on NCI-60 Panel
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
Pages
13
From page
953
To page
965
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
Journal title
Astroparticle Physics
Serial Year
2017
Record number
2416440
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