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Esters of Quinoxaline 1`4-Di--oxide with Cytotoxic Activity on Tumor Cell Lines Based on NCI-60 Panel. | LitMetric

Esters of Quinoxaline 1`4-Di--oxide with Cytotoxic Activity on Tumor Cell Lines Based on NCI-60 Panel.

Iran J Pharm Res

Departamento de Inmunología, Escuela Nacional de Ciencias Biológicas, Instituto Politécnico Nacional, Ciudad de México, México.

Published: January 2017

AI Article Synopsis

Article Abstract

Quinoxalines display diverse and interesting pharmacological activities as antibacterial, antiviral, antiparasitic and anticancer agents. Particularly, their 1`4-di--oxide 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--oxide substitutes at 7-position with esters group were synthetized and characterized by infrared (IR), proton nuclear magnetic resonance (H-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.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5610751PMC

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