Esters of Quinoxaline 1ˏ4-Di-<i>N</i>-oxide with Cytotoxic Activity on Tumor Cell Lines Based on NCI-60 Panel

AuthorGildardo Riveraen
AuthorSyed Shoaib Ahmad Shahen
AuthorDaniel Arrieta-Baezen
AuthorIsidro Palosen
AuthorAntonio Mongueen
AuthorLuvia Enid Sánchez-Torresen
Issued Date2017-07-31en
AbstractQuinoxalines 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
DOIhttps://doi.org/10.22037/ijpr.2017.2065en
KeywordAntitumoren
KeywordCanceren
KeywordDrugsen
KeywordEstersen
KeywordQuinoxaline 1en
Keyword4-di-<i>N</i>-oxideen
PublisherBrieflandsen
TitleEsters of Quinoxaline 1ˏ4-Di-<i>N</i>-oxide with Cytotoxic Activity on Tumor Cell Lines Based on NCI-60 Panelen
TypeOriginal Articleen

Files

Original bundle

Now showing 1 - 1 of 1
Loading...
Thumbnail Image
Name:
ijpr-16-0953.pdf
Size:
408.81 KB
Format:
Adobe Portable Document Format
Description:
Article/s PDF