两类氮芥衍生物的合成及其生理活性研究

Synthesis and Biological Activity of Two Kinds of Nitrogen Mustard Derivatives

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.