氮杂香豆雌酚衍生物的合成及其抗肿瘤活性  

Synthesis and Preliminary Antitumor Activities of Aza-coumestrol Derivatives

作　　者：董见生[1] 袁静梅[1] 何国学 潘成学[1] 苏桂发[1] 

机构地区：[1]广西师范大学省部共建药用资源化学与药物分子工程国家重点实验室,广西桂林541004

出　　处：《合成化学》2016年第9期774-779,共6页Chinese Journal of Synthetic Chemistry

基　　金：国家自然科学基金资助项目(21162002;21462008);广西自然科学基金资助项目(2014GXNSFAA118053;2015GXNSFDA139009);药用资源化学与药物分子工程教育部重点实验室基金资助项目(CMEMR2012-A014;CMEMR2014-A01);广西医药产业人才小高地基金资助项目(1308)

摘　　要：以间苯二甲醚为原料,经碘代、偶联、胺解、分子内环化及脱甲醚环化共5步反应,合成9个氮杂香豆雌酚衍生物(6a^6i),其结构经~1H NMR,13C NMR和APCI-MS表征。采用MTT法研究了6对Hela、SKOV3、BEL-7404、Hep G2及A-549等癌细胞的体外生长抑制活性。结果表明:6h对SKOV3细胞的生长抑制活性最高,其IC50值为81.58μmol·L-1。Nine aza-coumestrol derivatives（6a ~ 6i） were obtained by 5 steps including iodination,coupled reaction,aminolysis,intramolecular cyclization and the demethyl-cyclization using 1,3-dimethoxy-benzene as starting material. The structures were characterized by1 H NMR,13 C NMR and APCI-MS. The in vitro anti-tumor activities of 6 against Hela,SKOV3,BEL-7404,Hep G2 and A-549 were investigated by MTT method. The results demonstrated that 6h exhibited better inhibition activity against SKOV3 with IC50 of 81. 58 μmol·L- 1.

关 键 词：香豆雌酚 天然产物结构改造 合成 抗肿瘤活性 

分 类 号：O625.5[理学—有机化学] O621.3[理学—化学]