三氮杂大环及其衍生物的合成与其生物活性  

Synthesis and Biological Activities of Triazacyclodecane and Its Derivatives

作　　者：周双生[1] 张群英[1] 鲁传华[1] 毕建宏[2] 

机构地区：[1]安徽中医学院药学院,合肥230031 [2]合肥师范学院化学系,合肥230061

出　　处：《应用化学》2009年第6期671-675,共5页Chinese Journal of Applied Chemistry

基　　金：国家自然科学基金(20071001)资助项目;安徽省教育厅自然科学基金项目(KJ2007B209);现代中药安徽省重点实验室项目资助

摘　　要：合成了一种新的1,4,7-三氮杂十环配体及其4种衍生物,通过元素分析、IR1、H NMR和MS光谱测试技术对其结构进行了表征。用人癌细胞Hela和HCT26对合成的目标化合物进行了生物活性研究。结果表明,所合成的化合物都有一定的抗肿瘤活性,并呈剂量效应关系,其中化合物4作用后的HCT26细胞呈现变性坏死的形态学改变,可明显诱导HCT26肿瘤细胞凋亡。A novel 1,4,7-triazacyclodecane and its 4 derivatives were synthesized. These compounds were characterized by elemental analysis, IR, ^1H NMR and MS techniques. The biological activities of these compounds were investigated against human cancer cells Hela and HCT26 . The results showed that all the compounds possess, to some extent, antitumor activities which change in dose dependent manner. After treatment with compound 4, the degeneration and necrosis of HCT26 cells occurred, showing that compound 4 has significant apoptotic effect on HCT26 cells.

关 键 词：氮杂大环 衍生物 合成 生物活性 

分 类 号：O624.6[理学—有机化学]