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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.
The design and synthesis of three nitrogen mustards and six naphthalimide-nitrogen mustard derivatives were confirmed by 1H NMR, 13C NMR, ESI-MS and elemental analysis.Using MTT [3- (4,5-dimethylthiazol -2-yl) -2,5-diphenyltetrazolium bromide] method was used to test the in vitro antitumor activity of nine compounds against HL-60, K562 and SMMC-7721 tumor cells. The results showed that all the target compounds exerted anti-tumor activity on HL-60 cells All showed good activity in vitro, and the activity of compound 5 was superior to the commercial drug melphalan.The selective test of normal cells and tumor cells showed that 5a had better selectivity to SMMC-7721 cells and better than the positive control Fallon.