二茂铁席夫碱的合成及细胞毒活性

Synthesis and Cytotoxic Activities of Ferrocene Schiff Bases

基于含氮杂环化合物的生物活性,尤其是1,2,4-三唑类化合物的特性,研究了二茂铁席夫碱对癌细胞的毒性.将二茂铁甲醛(或乙酰基二茂铁)与3-取代-4-氨基-1,2,4-三唑-5-硫酮(或酰肼)缩合,反应得到6个新的含二茂铁基的缩胺类席夫碱和4个酰腙类席夫碱.利用1H NMR、IR、MS和元素分析对化合物结构进行了表征.体外细胞测试结果表明,所有化合物对宫颈癌细胞(Hela)均有一定的抑制生长活性,而且杂环缩胺类席夫碱2的细胞毒活性要强于酰腙类席夫碱4.

Ferrocene and its derivatives reveal many special properties and they have been used in many areas.Nitrogen-containing heterocyclic ring compounds have good biological activities,especially,the 1,2,4-triazole derivatives have been given much attention in recent years.In order to evaluate the cytotoxic activity of ferrocene Schiff base in this paper,six novel ferrocene Schiff bases were synthesized through the reaction of ferrocene carboxaldehyde with 3-substituted-4-amino-1,2,4-triazole-5-thione and four new ferrocene acylhydrazone Schiff bases were also synthesized through the reaction of ferrocenecarboxaldehyde or acetylferrocene with acylhydrazine.Their structures were characterized by 1H NMR,IR,MS and element analysis.Their cytotoxic activities were evaluated in vitro by an 3-（4,5-dimethylthiazol-2-yl）-2,5-diphenyltetrazolium bromide（MTT） assay using human cervical cancer cells（Hela） and the results show that these compounds exhibited some cytotoxic activities against cancer cells.In addition,the results indicate that compound 2 presented stronger cytotoxic activities against cancer cells（Hela） than compound 4.