有机化学 ›› 2009, Vol. 29 ›› Issue (07): 1096-1099. 上一篇    下一篇

研究论文

异维A酸二茂铁基衍生物的合成及其细胞毒活性的研究

梁盛宗a ; 忻鼎丞a ; 龙伯华a; 向建南*,a,b,c   

  1. (a湖南大学化学化工学院 长沙 410082)
    (b湖南大学生物医学工程中心 长沙 410082)
    (c湖南大学化学生物传感与计量学国家重点实验室 长沙 410082)
  • 收稿日期:2008-11-17 修回日期:2008-12-17 发布日期:2009-07-22
  • 通讯作者: 向建南

Synthesis and Cytotoxic Activities of 13-cis-Retinoyl Ferrocene Derivatives

Liang, Shengzonga ; Xin, Dingchena; Long, Bohuaa ; Xiang, Jiannan*,a,b,c   

  1. (a College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082)
    (b Bio-medicine Engineering Center, Hunan University, Changsha 410082)
    (c State Key Laboratory of Chem/Biosensing and Chemometrics, Hunan University, Changsha 410082)
  • Received:2008-11-17 Revised:2008-12-17 Published:2009-07-22
  • Contact: Xiang, Jiannan

为降低异维A酸的毒副作用并提高其癌细胞毒活性以及增加其在生物体内的吸收, 通过Mitsunobu反应, 以高于80%的收率合成了8种新异维A酸二茂铁基衍生物, 并进行了结构表征与确认. 采用3-(4,5-二甲基噻唑-2)-2,5-二苯基四唑溴盐(MTT)法测试了它们对肺癌细胞(A549)等的癌细胞毒活性. 结果显示, 引入二茂铁基团后的异维A酸二茂铁基衍生物具有很好的癌细胞毒活性.

关键词: 异维A酸, 二茂铁衍生物, Mitsunobu反应, 细胞毒活性

In order to decrease toxicities of retinoids, enhance their physiological activities against cancer cells and increase absorbency in the organisms, eight novel 13-cis-retinoyl ferrocene derivatives were synthesized in yields higher than 80% through Mitsunobu reactions. Their structures were characterized and their cytotoxic activities were determined in vitro by an 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay using human cancer lines including A549 cells lines etc. Results showed that the 13-cis-retinoyl ferrocene derivatives modified by ferrocene groups exhibited excellent cytotoxic activities against cancer cells.

Key words: cytotoxic activity, ferrocene derivative, Mitsunobu reaction, 13-cis-retinoic acid