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以芳香氮芥N,N-二(2-氯乙基)-1,4-苯二胺为药效基团,4位取代的苯胺和α-萘胺为载体,通过尿素的连接方式,合成了5个芳胺类氮芥衍生物,所有化合物的结构经元素分析、1HNMR、13CNMR和MS测试确证。对K562(白血病细胞),B16(黑色素瘤)和CHO(中国仓鼠卵巢癌细胞)三种细胞模型进行了体外抗肿瘤活性测试,结果表明部分化合物的活性较N,N-二(2-氯乙基)-1,4-苯二胺有明显提高,其中化合物5e在一定的浓度范围内与商品药物美法仑相当。
Aromatic nitrogen mustard N, N-bis (2-chloroethyl) -1,4-phenylenediamine as a pharmacodynamic group, 4-substituted aniline and α-naphthylamine as a carrier through the urea connection, synthesis Five aromatic amine nitrogen mustard derivatives were obtained. The structures of all the compounds were confirmed by elemental analysis, 1HNMR, 13CNMR and MS tests. The in vitro antitumor activity test of three cell models of K562 (leukemia cell), B16 (melanoma) and CHO (Chinese hamster ovary cancer cell) showed that the activity of some compounds was higher than that of N, N-bis Yl) -1,4-phenylenediamine, with compound 5e being comparable to the commercial drug melphalan at a range of concentrations.