Zoology Department, Faculty of Science, Port Said University, Port Said 42526, Egypt.
Chemistry Department, Faculty of Science, Port Said University, Port Said 42526, Egypt.
Molecules. 2021 Mar 18;26(6):1706. doi: 10.3390/molecules26061706.
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.
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。
