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5-芳基-1-芳亚氨基-1-咪唑-2(3)-硫酮:合成与体外抗癌活性评价。

5-Aryl-1-Arylideneamino-1-Imidazole-2(3)-Thiones: Synthesis and In Vitro Anticancer Evaluation.

机构信息

Zoology Department, Faculty of Science, Port Said University, Port Said 42526, Egypt.

Chemistry Department, Faculty of Science, Port Said University, Port Said 42526, Egypt.

出版信息

Molecules. 2021 Mar 18;26(6):1706. doi: 10.3390/molecules26061706.

Abstract

A novel series of arylidene amino imidazole-2-thiones were synthesized, identified using IR, H-NMR, and C-NMR spectral data. Cytotoxic effect of the prepared compounds was carried out utilizing three cancer cell lines; MCF-7 breast cancer, HepG2 liver cancer, and HCT-116 colon cancer cell lines. Imidazole derivative was the most potent of all against three cell lines. DNA flow cytometric analysis showed that, imidazoles and exhibit pre-G1 apoptosis and cell cycle arrest at G2/M phase. The results of the VEGFR-2 and B-Raf kinase inhibition assay revealed that compounds and displayed good inhibitory activity compared with reference drug erlotinib.

摘要

合成了一系列新型芳基亚氨基咪唑-2-硫酮,并通过红外光谱(IR)、氢核磁共振谱(H-NMR)和碳核磁共振谱(C-NMR)数据进行了鉴定。利用 MCF-7 乳腺癌、HepG2 肝癌和 HCT-116 结肠癌三种癌细胞系进行了所制备化合物的细胞毒性作用实验。咪唑衍生物 对三种细胞系的抑制活性最强。DNA 流式细胞术分析表明,咪唑 和 诱导细胞发生 G2/M 期细胞周期阻滞和 Pre-G1 期凋亡。VEGFR-2 和 B-Raf 激酶抑制实验的结果表明,与对照药物厄洛替尼相比,化合物 和 显示出良好的抑制活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8efb/8003321/b417957b0050/molecules-26-01706-g001.jpg

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