Synthesis and Biological Evaluation of SomeN-Substituted Quinoxaline Derivatives as Antitumor Agents

被引：16
作者：
Gobouri, Adil A. [1 ]
机构：
[1] Taif Univ, Dept Chem, Fac Sci, POB 888, Al Haweiah 21974, Taif, Saudi Arabia
来源：
RUSSIAN JOURNAL OF BIOORGANIC CHEMISTRY | 2020年 / 46卷 / 03期
关键词：
quinoxaline; anti-proliferative; cell cycle analysis; caspase; 3; 7; cisplatin; ANTICANCER; INHIBITORS;
D O I：
10.1134/S1068162020030097
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
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,H-1 NMR,C-13 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.
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页码：409 / 416
页数：8
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