摘要
设计合成了3个苯胺氮芥和6个萘酰亚胺-氮芥衍生物,产物结构均经1H NMR,13C NMR,ESI-MS和元素分析确认.使用MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide]法测试了9个化合物对HL-60,K562和SMMC-7721三种肿瘤细胞的体外抗肿瘤活性,测试结果表明所有目标化合物对HL-60细胞均具有较好的体外活性,其中化合物5活性优于商品药物美法仑.正常细胞和肿瘤细胞的选择性测试表明,5a对SMMC-7721细胞有较好的选择性,且优于阳性对照物美法仑.
Three aniline nitrogen mustard and six naphthalimide-nitrogen mustard derivatives were designed and synthesized. The structures of the synthesized compounds were confirmed by 1H NMR, 13C NMR, ESI-MS techniques and elemental analysis. The prelimilary antitumor activity was evaluated on HL-60, K562 and SMMC-7721 cell lines by MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] assay. The results demonstrated that target compounds exhibited antitumor activity for HL-60 and the activity of compound 5 was superior to commercial drug melphalan. Besides, the activity of compound 5a against SMMC-7721 cells is more selectivity than that of QSG-7701 cell lines.
出处
《有机化学》
SCIE
CAS
CSCD
北大核心
2011年第7期1122-1126,共5页
Chinese Journal of Organic Chemistry
基金
河南省科技厅基础与前沿(No.082300423203)
国家自然科学基金重大研究计划培育(No.90913001)资助项目
关键词
氮芥衍生物
合成
生理活性
nitrogen mustard derivative
synthesis
biological activity