氮杂环丁烷衍生物的合成及其抗肿瘤活性  

Synthesis and Cytotoxic Activities of Azetidine Derivatives

作　　者：赵淑艳[1] 左爱学[2] 毛泽伟[2] 

机构地区：[1]承德护理职业学院,河北承德067000 [2]云南中医学院中药学院,云南昆明650500

出　　处：《合成化学》2016年第9期785-788,793,共5页Chinese Journal of Synthetic Chemistry

基　　金：云南省应用基础研究计划资助项目(2015FB155)

摘　　要：以3-羟基氮杂环丁烷盐酸盐为原料,经取代、官能团转化制得3-氨基氮杂环丁烷化合物(3);3经衍生化合成了10个3-氨基氮杂环丁烷衍生物(4a^4j),其中4f^4j为新化合物,其结构经1H NMR,13C NMR和HRMS(ESI-TOF)表征。采用MTT法初步测试了化合物的体外抗肿瘤活性。结果表明:4h对A549表现出较强的细胞毒活性(IC50=8.06μmol·L^(-1))。4-（3-aminoazetidine-1-yl） acetophenone（3） was synthesized by substitution and functional transformation using 3-hydroxyazetidine hydrochloride as starting material. Ten 3-aminoazetidine derivatives（4a ~ 4j） were synthesized by derivatization of 3. Among them,4f ~ 4j were novel compounds.The structures were characterized by1 H NMR,13 C NMR and HR-MS（ESI-TOF）. The preliminary cytotoxic activities were studied in vitro against a panel of human tumor cell lines（Hela,A549） by the MTT assay. The result indicated that compound 4h was found to be the most potent compound against A549（IC50= 8. 06 μmol·L- 1）.

关 键 词：3-羟基氮杂环丁烷 氮杂环丁烷 衍生物 合成 抗肿瘤活性 

分 类 号：O625.42[理学—有机化学]