应用化学 ›› 2009, Vol. 26 ›› Issue (6): 671-675.

• 研究论文 • 上一篇    下一篇

三氮杂大环及其衍生物的合成与其生物活性

周双生   

  1. 安徽中医学院药学院
  • 收稿日期:2008-05-23 修回日期:2008-07-22 出版日期:2009-06-10 发布日期:2009-06-10
  • 通讯作者: 周双生
  • 基金资助:
    安徽省教育厅自然科学基金

Synthesis and Biological Activities of Triazacyclodecane and Its Derivative

  • Received:2008-05-23 Revised:2008-07-22 Published:2009-06-10 Online:2009-06-10

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,IR,1HNMR和MS光谱对其结构进行了表怔。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。

关键词: 氮杂大环, 衍生物, 合成, 生物活性, 氮杂大环, 衍生物, 合成, 生物活性

Abstract:

A novel 1,4,7-triazacyclodecane and its 4 derivatives were synthesized. These cmpounds were characterized by elemental analysis,IR,1HNMR and MS spectra. The biological activities of these cmpounds had been investigated in human cancer cell Hela and HCT26 . The results showed that all compounds possessed some extent antitumor activities which were in dose dependent manner.After treatment with compound 4 ,the changes of degeneration and necrosis occurred in HCT26 cells,had significantly apoptotic effect on HCT26 cells.

Key words: azamacrocycle, derivative, synthesis, biological activity