Synthesis of novel,azasugar-modified anthraquinone derivatives and their cytotoxicity

A series of novel, azasugar-modified 2-monosubstituted, 2,6- and 2,7-bissubstituted anthraquinone derivatives have been synthesized by the nucleophilic substitution of N-alkylamino azasugar with mono-, bis（2-chloroacetamido）anthraquinones. Their cytotoxic activities against HeLa and MCF-7 ceils were preliminarily evaluated and compound 9a with mono-azasugar pendant at 2-position showed similar activity to the control drug （Cisplatin）.     

微波促进立体选择性合成烯丙酸酯类高碳糖衍生物

在微波促进下, 利用酮糖(1)及糖酸内酯(4)与叶立德(2, Ph₃PCHCOOEt)的Wittig反应, 立体选择性地合成了糖基烯丙酸酯类化合物(3和5), 反应效率显著提高, 反应时间由原来的20 h缩短为10 min; 并且研究了不同反应溶剂对反应立体选择性的影响. 提供了一种高效、 简便合成含有烯丙酸酯类高碳糖衍生物的方法.     

溴代1,4,5,8-萘四甲酸酐的选择性合成

在常压下, 以溴化钠和发烟硫酸(含质量分数为40%的SO₃)为溴化试剂, 通过控制反应温度、 反应时间和溴化钠的投料比选择性地合成了2-溴-1,4,5,8-萘四甲酸酐和2,6-二溴-1,4,5,8-萘四甲酸酐. 本研究提供了一种合成溴代1,4,5,8-萘四甲酸酐衍生物的新方法.     

The synthesis and biological activity of novel spiro-isoxazoline C-disaccharides based on 1,3-dipolar cycloaddition of exo-glycals and sugar nitrile oxides

A series of novel spiro-isoxazoline C-disaccharides were synthesized by the key step of 1,3-dipolar cycloaddition reactions of exo-glycals and sugar nitrile oxides, and followed by catalytic debenzylation in the presence of Pd(OH)₂/C. The cycloaddition reactions were carried out stereoselectively and afforded α-isomers exclusively except in the case of galactose. The biological activities of the novel disaccharides against the glycosidases (α-amylase, α-glucosidase, and β-glucosidase) and HIV and BVDV were evaluated.     

微波促进1,3-偶极环加成反应合成氮杂糖苷衍生物

利用微波促进氮杂糖硝酮(2)与丙烯酸类衍生物(3)发生1,3-偶极环加成反应,立体选择性地得到了一系列新的含异噁唑烷的氮杂糖衍生物(4),反应效率显著提高,反应时间由95h缩短为5～15min,收率由67%提高到78%～88%.利用NMR和HRMS等方法结合化合物(4d-1)的单晶结构确定了产物的结构和相对构型.     

Cytotoxic activity and DNA binding of naphthalimide derivatives with amino acid and dichloroacetamide functionalizations

A series of novel naphthalimide derivatives modified by amino acids and their dichloroacetamide derivatives at the 3-position have been synthesized. Their cytotoxic activities were preliminarily evaluated against Hela, A549 and K562 cells, which showed that the length of the side chains of the amino acids influenced the cytotoxic activities. Moreover, compound 7d showed a very good cytotoxic activity against A549 cells with an IC50 value of 4.78 mmol Là1. Furthermore, the UV–vis, fluorescence,and circular dichroism(CD) spectroscopies and thermal denaturation experiment indicated that compounds 6a, 6d and 7a, 7d, as DNA intercalators, exhibited binding affinities with calf-thymus DNA(Ct-DNA).     

五元氮杂糖衍生物的实用有效合成方法

以D-葡萄糖为原料, 经具有降冰片烷结构的双环缩醛中间体, 合成了部分羟基保护的1-脱氧-D-氮杂阿拉伯糖衍生物, 提供了一种合成五元氮杂糖衍生物的简便有效方法.