作　　者： (周楠）; (冯甜）; (刘畅）; (吴让鑫）; (崔家辉）; (张生勇）; (陈惠）;

机构地区： 第四军医大学药学院药物化学教研室,陕西西安710032

出　　处： 《中国药物化学杂志》 2017年第4期261-266,共6页

摘　　要： 目的设计合成系列芳基磺酰胺类化合物,并评价其辐射防护活性。方法以市售1,8-二萘甲酸酐为起始原料,通过胺化反应及两步霍夫曼烷基化反应得到目标化合物。采用MTT法检测目标化合物对人脐静脉内皮细胞(Huvecs)和人正常肝细胞(L-02)的毒性及辐射防护活性。结果与结论合成得到6个结构全新的芳基磺酰胺类化合物,其结构经~1H-NMR、^(13)C-NMR及HR-MS进行确认。其中,化合物7b对Huvecs和L-02两种细胞的毒性小(IC50值分别为197.8μmol·L^(-1)和195.1μmol·L^(-1)),且能显著改善两种辐射损伤细胞的增殖能力,有进一步研究的价值。 The compound SBA specially working to the LPA2 receptor shows perfect anti-radiation activities. In order to further improve the anti-radiation activity,a number of novel arylsulfonamides were designed. Six target compounds were synthesized from 1,8-naphthalic anhydride via 3-step reactions containing amination and twice N-alkylation. Their structures were characterized by ~1H-NMR,^（13）C-NMR and HR-MS.The cytotoxicity in human umbilical vein endothelial cells（ Huvecs） and L-02 cells in vitro were tested by MTT assay. Among them,compound 7b shows lowcytotoxicity against Huvecs and L-02 cells with IC50 values of 197. 8 μmol·L^（-1）,195. 1 μmol·L^（-1）,respectively. And the anti-radiation activity assay shows compound 7b has the best effect on improving the multiplication capacity of damaged cells. Therefore,7b may be a potential anti-radiation agent and valuable for further investigation.

关 键 词： 苯基磺酰胺 合成 辐射防护活性