Luo Wen, Zhao Yong-mei, Wang Yu-xia, Xie Song-qiang, Zhao Jin, Wang Chao-jie
Institute of Natural Products, College of Chemistry and Techonology, Henan University, Kaifeng 475001, China.
Yao Xue Xue Bao. 2007 Dec;42(12):1327-9.
To study the effect of isoprenoid and aliphatic saturated alcohols as modificator on benzoic nitrogen mustard, the intermediate 4-[N,N-bis(2-chloroethyl) amino] benzoic acid 4 was prepared in four steps utilizing p-amino benzoic acid as the starting material. Target compounds were synthesized by the catalytic esterification of DCC/DMAP and the structures of the six new esters were characterized by elemental analysis, 1H NMR, 13C NMR and MS. Antitumor activities were evaluated in vitro using MTT assay. The result showed that some derivatives were more potent than the intermediate 4, and compound 5c modified with dodecanol exhibited similar activity to the commercial drug melphalan.
为研究类异戊二烯和脂肪族饱和醇作为修饰剂对苯甲酸氮芥的影响，以对氨基苯甲酸为起始原料，经四步反应制备了中间体4-[N,N-双(2-氯乙基)氨基]苯甲酸4。通过DCC/DMAP催化酯化反应合成了目标化合物，并用元素分析、1H NMR、13C NMR和MS对六种新酯的结构进行了表征。采用MTT法体外评价了其抗肿瘤活性。结果表明，一些衍生物比中间体4更具活性，用十二醇修饰的化合物5c表现出与市售药物美法仑相似的活性。
