三氮杂十环及其铂(II)配合物的合成以及抗肿瘤活性  

Synthesis and antitumor activities of triazacyclodecane and its platinum(II) complex

作　　者：周双生[1] 张群英[1] 秦凯[1] 鲁传华[1] 谢复新[2] 

机构地区：[1]安徽中医学院药学院,安徽合肥230031 [2]安徽大学化学化工学院

出　　处：《药学学报》2008年第5期490-494,共5页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金资助项目(29871001);安徽省教育厅自然科学基金资助项目(KJ2007B209);安徽省药用基础化学重点实验室资助项目.

摘　　要：为了寻找具有优良高效低毒的抗肿瘤药物,合成了一种新的1,4,7-三氮杂十环配体及其铂(II)配合物,并经元素分析、IR、1H NMR、13C NMR、MS谱、差热分析和电导方法表征。体外生物活性表明这些化合物具有较强的抗肿瘤活性;用抑瘤率和相对生长率测定了人肝瘤(CA)的抑制作用,体内试验显示铂(II)配合物(C)具有抗人肝癌瘤(CA)作用。其中剂量为12 mg.kg-1抗瘤活性与对照药相当,它的半数致死量为853.6 mg.kg-1。To search for potential antitumor drugs with potent efficiency and low toxicity, a novel 1,4,7-triazacyclodecane and its platinum （Ⅱ） complex were synthesized. These compounds were characterized by elemental analysis, IR, ^1H NMR, ^13C NMR, MS spectra, thermoanalysis and conductivity measurement. Antitumor activity study indicated these compounds had strong antitumor activity in vitro to some extent. Inhibition of human liver tumor of CA was examined by antitumor rate and growth rate, complex C showed inhibition activity on transplanting-tumor growth of CA, 12 mg ·kg^-1 was as potent as cisplatin, its ID50 was 853.6 mg · kg^-

关 键 词：氮杂大环 配合物 合成 抗肿瘤活性 

分 类 号：R916.2[医药卫生—药学]