几类席夫碱衍生物的合成及抗肿瘤活性研究
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摘要
研究发现,席夫碱类化合物以其较强的配位能力、良好的生物药理活性以及其它方面的优越性能,使其成为很有潜力的治疗药物和功能材料。为了进一步研究这些化合物的抗肿瘤活性,合成了一系列席夫碱类化合物。
     本文合成了酰腙、缩胺硫脲、肼基二硫代甲酸甲酯和氨基三氮唑类席夫碱衍生物,共36个。通过红外光谱、质谱和核磁共振氢谱确证了化合物的结构,培养得到一个化合物的单晶,并用X射线单晶衍射仪测定了晶体结构。
     将化合物V1和V2进行了抗肿瘤生物活性体外筛选实验。结果表明:这两个化合物对人肝癌SMMC7721细胞和人结直肠癌COL0205细胞具有强体外增殖抑制作用,其IC_(50)均小于1μmol/L。所合成的部分化合物在分析化学上的应用及生物活性试验正在进行中。
According to the literature,it is found that Schiff bases have strong coordination ability,good biological activities and other excellent properties,which make them potential drugs and functional materials.For further researching their anticancer activity,a series of Schiff base derivatives were synthesized.
     A total of 36 compounds,including acylhydrazones,thiosemicarbaz -ones,methyl hydrazinecarbodithioate and aminotriazole Schiff bases, were synthesized and characterized by IR,MS and ~1HNMR.The crystal structure of one compound was determined by single crystal X-ray diffraction analysis.
     Antitumor activity of some compounds have also been investigated. The results show that both V1 and V2 have excellent inhibitory effect on SMMC7721 and COLO205 cell growth.The IC_(50) values(72h) of V1 and V2 on SMMC7721 and COLO205 cells are no more than 1μmol/L, respectively.The bioactivities and applications of other compounds on analytical chemistry are being carried on.
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