新型5-氢磺酰基-1H-苯并[d]咪唑-2(3H)-酮衍生物的合成与抗肿瘤评价
Synthesis and Antitumor Evaluation of Novel 5-Hydrosulfonyl-1H-benzo[d]imidazol-2(3H)-one Derivatives.
作者信息
Ouyang Guang, Tong Rongsheng, Li Jinqi, Bai Lan, Ouyang Liang, Duan Xingmei, Li Fengqiong, He Pin, Shi Jianyou, He Yuxin
机构信息
Individualized Medication Key Laboratory of Sichuan Province, Sichuan Academy of Medical Science & Sichuan Provincial People's Hospital, Chinese Academy of Sciences Sichuan Translational Medicine Research Hospital, School of Medicine, Center for Information in Medicine, University of Electronic Science and Technology of China, Chengdu 610072, Sichuan, China.
State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu 610041, Sichuan, China.
出版信息
Molecules. 2016 Apr 20;21(4):516. doi: 10.3390/molecules21040516.
A series of novel 5-hydrosulfonyl-1H-benzo[d]imidazol-2(3H)-one derivatives bearing natural product substructures has been successfully synthesized and their antitumor activity studied. These newly synthesized derivatives were characterized by ¹H-NMR, (13)C-NMR and high resolution mass spectral data, then screened as antitumor agents against the A549, HCC1937, and MDA-MB-468 human tumor cell lines using MTT cell proliferation assays. The results show that some of these compounds can effectively inhibit the growth of these cancerous cells, with compound 5b being the best one (IC50 = 2.6 μM). Flow cytometry data revealed that compound 5b induced apoptosis of HCC1937 cells with increased solution concentration. The structure and activity relationships (SAR) of these compounds is summarized.
一系列带有天然产物亚结构的新型5-氢磺酰基-1H-苯并[d]咪唑-2(3H)-酮衍生物已成功合成，并对其抗肿瘤活性进行了研究。这些新合成的衍生物通过¹H-NMR、(13)C-NMR和高分辨率质谱数据进行表征，然后使用MTT细胞增殖试验作为抗肿瘤剂对A549、HCC1937和MDA-MB-468人肿瘤细胞系进行筛选。结果表明，其中一些化合物可以有效抑制这些癌细胞的生长，化合物5b表现最佳（IC50 = 2.6 μM）。流式细胞术数据显示，化合物5b随着溶液浓度的增加诱导HCC1937细胞凋亡。总结了这些化合物的构效关系（SAR）。
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