氮杂香豆雌酚衍生物的合成及其抗肿瘤活性

摘要

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-dime-thoxy-benzene as starting material .The structures were characterized by 1 H NMR, 13 C NMR and AP-CI-MS.The in vitro anti-tumor activities of 6 against Hela, SKOV3, BEL-7404, HepG2 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 .%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、HepG2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.