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

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.