2-吡唑啉衍生物的合成及其对白血病癌症细胞株K562细胞毒性的评价

M. Shaabanzadeh, M. Torbati
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引用次数: 1

摘要

2-吡唑啉衍生物具有广泛的生物作用,如抗病毒、抗菌、抗真菌、抗抑郁和抗癌作用。研究表明,含有2-吡唑啉和其他杂环的化合物可能显示出更有效的生物特性。本研究采用一锅微波辅助法合成了一种C3位具有螺茚基喹喔啉环的2-吡唑啉衍生物,并通过1H NMR光谱证实了其化学结构。用MTT法评价该化合物对K562细胞系和植物血凝素活化的外周血单个核细胞(PHA+PBMC)的细胞毒作用。此外,还研究了顺铂对这些细胞的细胞毒性作用,并与2-吡唑啉的细胞毒性进行了比较。IC50值​​2-吡唑啉衍生物对K562细胞系和PHA+PBMC细胞的作用分别为45和55μg/mL,而顺铂抑制相同细胞的增殖的IC50值分别为1.71和7.8μg/mL。本研究的结果表明,合成的衍生物在比顺铂更高的浓度下对K562癌症细胞系具有细胞毒性活性。
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Synthesis and Cytotoxic Evaluation of 2-Pyrazoline Derivative on Leukemia Cancer Cell Line K562
The 2-pyrazoline derivatives have a wide range of biological effects, such as anti-viral, anti-bacterial, anti-fungal, anti-depressant and anti-cancer effects. Studies have shown that compounds containing 2-pyrazoline along with another heterocycles may show more effective biological properties. In this study, a 2-pyrazoline derivative with a spiro-indenoquinoxaline ring at C3 position was synthesized by one-pot microwave-assisted method and its chemical structure was confirmed by 1H NMR spectroscopy. The cytotoxic effects of the compound were evaluated on the K562 cell line and phytohemagglutinin-activated peripheral blood mononuclear cells (PHA+PBMC) by MTT assay. Additionally, the cytotoxic effects of cisplatin on these cells were investigated and compared with those of 2-pyrazoline. The IC50 values ​​obtained from the 2-pyrazoline derivative effects on the K562 cell line and PHA+PBMC cells were 45 and 55 μg/mL respectively, while cisplatin inhibited proliferation of the same cells with IC50 value 1.71 and 7.8 µg/mL respectively. The results of this study showed that the synthesized derivative had a cytotoxic activity on the K562 cancer cell line at higher concentrations than cisplatin.
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来源期刊
Journal of Chemical Health Risks
Journal of Chemical Health Risks Environmental Science-Health, Toxicology and Mutagenesis
CiteScore
1.30
自引率
0.00%
发文量
0
审稿时长
3 weeks
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