Synthesis, cytotoxicity and apoptosis‐inducing activity of novel 1H‐benzo[d]imidazole derivatives of dehydroabietic acid,Journal of the Chinese Chemical Society

当前位置： X-MOL 学术 › J. Chin. Chem. Soc. › 论文详情

Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)

Synthesis, cytotoxicity and apoptosis‐inducing activity of novel 1H‐benzo[d]imidazole derivatives of dehydroabietic acid
Journal of the Chinese Chemical Society ( IF 1.6 ) Pub Date : 2020-07-28 , DOI: 10.1002/jccs.202000075
A‐Liang Li ₁ , Ya‐Qun Yang ₁ , Wen‐Yan Wang ₁ , Qing‐Song Liu ₁ , Yue Sun ₁ , Wen Gu ₁

Affiliation

With the expectation of finding new and effective antitumor drugs, a series of novel N‐(1H‐benzo[d]imidazole‐2‐yl)‐benzamide/benzenesulfonamide derivatives of dehydroabietic acid were synthesized and evaluated for cytotoxic activity against three human cancer cell lines (MCF‐7, HeLa, and HepG2 cells) and one human normal hepatocyte cell line (LO2). As a result, a number of derivatives showed moderate to good antitumor activities. Among them, compound 8h exhibited the most potent activities against three cancer cell lines with IC₅₀ values of 0.87 ± 0.18, 9.39 ± 0.72, and 8.31 ± 0.64 μM, respectively, and was less active to normal hepatocyte LO2 cells. Further mechanism studies revealed that compound 8h could arrest the cell cycle of MCF‐7 cells at S phase and induce the apoptosis of MCF‐7 cells in ROS‐mediated mitochondrial pathway.

中文翻译：

新型脱氢松香酸的1H-苯并[d]咪唑衍生物的合成，细胞毒性和诱导凋亡的活性

期望找到新的有效的抗肿瘤药物，合成了一系列新型的脱氢松香酸N-（1H-苯并[ d ]咪唑-2-基）苯甲酰胺/苯磺酰胺衍生物，并评估了其对三种人类癌症的细胞毒活性。细胞系（MCF-7，HeLa和HepG2细胞）和一种人类正常肝细胞系（LO2）。结果，许多衍生物显示出中等至良好的抗肿瘤活性。其中，化合物8h对三种癌细胞株表现出最有效的活性，IC ₅₀值分别为0.87±0.18、9.39±0.72和8.31±0.64μM，对正常肝细胞LO2细胞的活性较低。进一步的机理研究表明，该化合物8h可阻止MCF-7细胞在S期的细胞周期，并诱导ROS介导的线粒体途径中MCF-7细胞的凋亡。

更新日期：2020-09-24

点击分享查看原文

点击收藏

阅读更多本刊最新论文本刊介绍/投稿指南11