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Synthesis and Biological Evaluation of Some N-Substituted Quinoxaline Derivatives as Antitumor Agents
Russian Journal of Bioorganic Chemistry ( IF 1.1 ) Pub Date : 2020-05-01 , DOI: 10.1134/s1068162020030097
Adil A. Gobouri

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.

中文翻译:

一些作为抗肿瘤剂的 N-取代喹喔啉衍生物的合成和生物学评价

通过在不同条件下将 3-羟基-2-氧代喹喔啉与 2,3-不饱和羰基化合物缩合,以产生酯和酰胺衍生物,合成了一种含有 1-(N-取代)-喹喔啉衍生物的新型杂化分子。所制备化合物的结构通过红外光谱、1H NMR、13C NMR、质量和元素分析进行​​了阐明。评估了所有制备的化合物对两种癌细胞系(MCF-7 和 Hela)的抗癌活性。3-(p-甲氧基苯基)-3-(3-羟基-2-氧喹喔啉-1-基)-2-氰基丙烯酸酰肼化合物的细胞周期分析表明细胞周期停滞在 S 期和 Pre-G1 细胞凋亡。DNA 合成抑制百分比表明,该化合物显示出与阿霉素等效的活性。此外,
更新日期:2020-05-01
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