萘酰亚胺-多胺缀合物的合成、生物活性和荧光光谱  

Synthesis,Biological Activitity and Fluorescence Spectroscopy of Naphthalimide-polyamine Conjugates

作　　者：田智勇[1] 苏雷朋[1] 谢松强[1] 赵瑾[1,2] 王超杰[1,2] 

机构地区：[1]河南大学化学生物学研究所,开封475004 [2]河南大学天然药物与免疫工程重点实验室,开封475004

出　　处：《有机化学》2013年第7期1514-1521,共8页Chinese Journal of Organic Chemistry

基　　金：中国博士后科学基金(No.20110490991);河南省自然科学(No.112300410181);河南省科技攻关(No.132102310026);河南省教育厅自然科学基金(No.2011B3500001)资助项目~~

摘　　要：合成了9个新的萘酰亚胺-多胺缀合物,化合物的结构经元素分析,1H NMR,13C NMR和MS确证.经MTT[3-(4,5-二甲基噻唑-2)-2,5-二苯基四氮唑溴盐]法对白血病细胞(K562)、人乳腺癌细胞(MB-231)和肝癌细胞(7721)体外活性测试.结果显示多数化合物对肿瘤细胞具有抑作用,尤其是化合物5a的抗肿瘤活性优于处于III期临床试验阶段药物氨萘非特(Amonafide).化合物5a与鲱鱼精DNA-EB作用的荧光光谱研究提示:DNA-EB与萘酰亚胺-多胺作用引起的荧光淬灭机制属于静态淬灭,DNA与萘酰亚胺-多胺物结合模式是扦插结合.Nine novel naphthalimide-polyamine conjugates were synthesized and their structures were confirmed by elemen- tal analysis, IH NMR, 13C NMR and MS techniques. Their antitumor activities in vitro using MTT [3-（4,5-dimethylthiazol- 2-yl）-2,5-diphenyltetrazolium bromide] assay were assessed on leukemia cells （K562）, human breast cancer cells （MB-231） and human hepatoma cells （7721）. The results showed that most of them exhibited antitumor activities. Especially, compound 5a was better than amonafide which has been in phase III clinical trials. Fluorescence data revealed that the fluorescence quenching of herring sperm DNA-EB complex by compound 5a was a static quenching type and naphthalimide-polyamine conjugates intercalate into the DNA base pairs.

关 键 词：萘酰亚胺 多胺缀合物 合成 抗肿瘤活性 荧光光谱 

分 类 号：TQ463[化学工程—制药化工]