摘要
研究表明,席夫碱类化合物具有良好的抗肿瘤生物活性.以氮杂靛红及其衍生物、水合肼为原料,合成了一系列对称双氮杂靛红席夫碱,并对合成的化合物进行了结构表征与初步的抗肿瘤活性测试.结果显示所合成化合物对不同的肿瘤细胞株表现出不同程度的抑制作用,其中化合物1、6、7、11、12、18、19的活性较好,尤其是对HepG_2细胞株的抑制活性较高.在此基础上,进一步研究了不同取代基对氮杂靛红席夫碱抗肿瘤活性的影响,总结了构效关系,结果发现在卤素取代的氮杂靛红母核能提高氮杂靛红席夫碱类化合物的抗肿瘤活性.本研究为为氮杂靛红席夫碱类化合物二次优化和进一步获得候选药物有提供了重要的依据.
Studies showed that the schiff base compounds had significant antitumor activities. In order to further enrich and extend the research of schiff base, a seriesschiff base of nitrogen heterocyclic isatin as well as derivatives have been synthesized with hydrazine hydrate,the structure of the compounds were characterized by NMR and HRMS. Additionally, the antitumor activity of the synthesized compounds have also been preliminari-ly investigated by MTT method. The results revealed that these compounds have moderate to intensive antitumor activities on different cell lines, specitically,compounds 1,6,7,1 1,1 2,18, 19 have stronger activities on HepG2 cells. The effect of nitrogen heterocyclic isatin substituents on antitumor activity has also been studied, which indicated that halogthe antitumor activity of synthesized compounds. In brief,our research can provide an experimental basis for the further synthesis and screening of candidate compounds.
出处
《陕西科技大学学报（自然科学版）》
2016年第4期136-144,共9页
Journal of Shaanxi University of Science & Technology
基金
陕西省教育厅专项科研计划项目(15JK1076)
陕西省人力资源与社会保障厅博士后基金项目(2015)
关键词
氮杂靛红
席夫碱
抗肿瘤
药物合成
nitrogen heterocyclic isatin
schiff base
antitumor activity
drug synthesis
