N-取代二苯并[a,j]呫吨-3,11-二甲酰胺衍生物的合成及其细胞毒性
Synthesis and Cytotoxicity of N-Substituted Dibenzo[a,j]xanthene-3,11-dicarboxamide Derivatives.
作者信息
Song Yongbin, Yang Yihui, Wu Lijun, Dong Naiwei, Gao Shang, Ji Hongrui, Du Xia, Liu Bo, Chen Guoyou
机构信息
School of Chemical and Environmental Engineering, Harbin University of Science and Technology, Harbin 150040, China.
College of Pharmacy, Harbin Medical University, Harbin 150081, China.
出版信息
Molecules. 2017 Mar 23;22(4):517. doi: 10.3390/molecules22040517.
In order to study the structure-activity relationships of xanthene derivatives, four series of -substituted 14-aryl-14-dibenzo[,]xanthene-3,11-dicarboxamide derivatives were synthesized. The structures of all compounds were identified by ¹H-NMR, HR-MS and IR spectra, in which compounds 6a-h were further identified by C-NMR spectra. The in vitro antitumor activity of the synthesized compounds was tested by MTT assay. Most of them displayed strong inhibitory activity on human hepatocellular carcinoma cell lines (SK-HEP-1, HepG2 and SMMC-7721 cells) and acute promyelocytic leukemia NB4 cells. Compounds - exhibited significant inhibitory activity against NB4 cells with IC values of 0.52 μM and 0.76 μM, respectively, much lower than 5.31 μM of the positive control As₂O₃.
为了研究呫吨衍生物的构效关系，合成了四个系列的β-取代的14-芳基-14-二苯并[,]呫吨-3,11-二甲酰胺衍生物。所有化合物的结构通过¹H-NMR、HR-MS和IR光谱进行鉴定，其中化合物6a-h进一步通过¹³C-NMR光谱进行鉴定。通过MTT法测试了合成化合物的体外抗肿瘤活性。它们中的大多数对人肝癌细胞系（SK-HEP-1、HepG2和SMMC-7721细胞）和急性早幼粒细胞白血病NB4细胞表现出较强的抑制活性。化合物-对NB4细胞表现出显著的抑制活性，IC值分别为0.52 μM和0.76 μM，远低于阳性对照As₂O₃的5.31 μM。
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