Esters of Quinoxaline 1,4-di-N-oxide with Cytotoxic Activity on Tumor Cell Lines Based on NCI-60 Panel

Iranian Journal of Pharmaceutical Research

关键词: Antitumor;    Cancer;    Drugs;    Esters;    Quinoxaline 1;    4-di-N-oxide;   

DOI  :  

学科分类：社会科学、人文和艺术（综合）

来源: Shaheed Beheshti Medical University * School of Pharmacy

【 摘 要 】

Quinoxalines display diverse and interesting pharmacological activities as antibacterial, antiviral, antiparasitic and anticancer agents. Particularly, their 1,4-di-N-oxides 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-N-oxides 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.

【 授权许可】

CC BY