Synthesis and Biological Evaluation of Some N-Substituted Quinoxaline Derivatives as Antitumor Agents
Adil A. Gobouri
Abstract
A new hybrid molecules containing 1-(N-substituted)-quinoxaline derivatives were synthesized from condensation of 3-hydroxy-2-oxo quinoxaline with 2,3-unsaturated carbonyl compounds under different conditions in order to yield ester and amide derivatives. The structure of the prepared compounds was elucidated on the bases of IR, 1H NMR, 13C NMR, mass and elemental analyses. All the prepared compounds were evaluated for their anticancer activity against two cancer cell line (MCF-7 and Hela). Cell cycle analysis of 3-(p-methoxyphenyl)-3-(3-hydroxy-2-oxoquinoxalin-1-yl)-2-cyanoacrylic acid hydrazides compound demonstrated cell cycle arrest at S phase and Pre-G1 apoptosis. DNA synthesis inhibitory percentage revealed that this mentioned compound showed equipotent activity to Doxorubicin. Additionally, apoptosis was confirmed by increase the percentage of caspase 3/7 higher than Cisplatin.