Wang Zhe, Deng Xiangping, Xiong Shujuan, Xiong Runde, Liu Juan, Zou Liu, Lei Xiaoyong, Cao Xuan, Xie Zhizhong, Chen Yanming, Liu Yunmei, Zheng Xing, Tang Guotao
a Institute of Pharmacy and Pharmacology, Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study , University of South China , Hengyang , China.
b Mu Dan Jiang You Bo Pharmacertical Co. Ltd , Mudanjiang , China.
Nat Prod Res. 2018 Dec;32(24):2900-2909. doi: 10.1080/14786419.2017.1389940. Epub 2017 Oct 24.
A series of chrysin benzimidazole derivatives were synthesised and evaluated for their anticancer activity in the search for potential anticancer agents. Among them, compound 18 displayed the most potent anti-proliferative activity against MFC cells with IC values of 25.72 ± 3.95 μM. The flow cytometry results displayed that compound 18 induced apoptosis of MFC cells in a dose-dependent manner and caused the cell cycle to be arrested in the G0/G1 phase. Furthermore, the preliminary anticancer activity in vivo was also studied in tumour-bearing mice, and the compound 18 exerted good inhibition effect on tumour growth. These results suggested that compound 18 had good anticancer activity, which could be a potential anticancer agent after further optimisation and evaluation.
合成了一系列白杨素苯并咪唑衍生物，并对其抗癌活性进行了评估，以寻找潜在的抗癌药物。其中，化合物18对MFC细胞表现出最强的抗增殖活性，IC值为25.72±3.95μM。流式细胞术结果显示，化合物18以剂量依赖的方式诱导MFC细胞凋亡，并使细胞周期停滞在G0/G1期。此外，还在荷瘤小鼠中研究了其体内初步抗癌活性，化合物18对肿瘤生长具有良好的抑制作用。这些结果表明，化合物18具有良好的抗癌活性，经过进一步优化和评估后可能成为一种潜在的抗癌药物。
