Esters of Quinoxaline 1ˏ4-Di-<i>N</i>-oxide with Cytotoxic Activity on Tumor Cell Lines Based on NCI-60 Panel
Author | Gildardo Rivera | en |
Author | Syed Shoaib Ahmad Shah | en |
Author | Daniel Arrieta-Baez | en |
Author | Isidro Palos | en |
Author | Antonio Mongue | en |
Author | Luvia Enid Sánchez-Torres | en |
Issued Date | 2017-07-31 | en |
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. | en |
DOI | https://doi.org/10.22037/ijpr.2017.2065 | en |
Keyword | Antitumor | en |
Keyword | Cancer | en |
Keyword | Drugs | en |
Keyword | Esters | en |
Keyword | Quinoxaline 1 | en |
Keyword | 4-di-<i>N</i>-oxide | en |
Publisher | Brieflands | en |
Title | Esters of Quinoxaline 1ˏ4-Di-<i>N</i>-oxide with Cytotoxic Activity on Tumor Cell Lines Based on NCI-60 Panel | en |
Type | Original Article | en |
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