【摘要】 采用苯甲醛和20(S)-喜树碱为原料,通过Minisci反应合成了7-苯甲酰基喜树碱。考察了影响该反应的因素,其优化条件为:喜树碱0.5 g,75%H2SO430 mL,苯甲醛1.5 mL,n(30%H2O2)∶n(FeSO4.7H2O)为20∶1,30%H2O21.0 mL,反应在0~2℃进行,反应时间6 h,产率可达58.2%。目标化合物采用MS1、H NMR及IR等手段进行了结构表征,并用SRB法在体外对人癌细胞增殖的抑制作用进行了初步测定,结果表明:该化合物对白血病(HL-60)、胃癌(BGC-823)、肝癌(Bel-7402)三种人癌细胞增殖都有抑制作用,尤其是对人胃癌BGC-823的抑制作用尤为突出,显示出良好的体外抗肿瘤活性。更多还原

【Abstract】 7-Benzoyl-camptothecin was synthesized from benzaldehyde and 20（S）-camptothecin by Minisci radical displace reaction.Optimum conditions for the reaction were found.When 0.5 g 20（S）-camptothecin,30 mL 75%H₂SO₄,1.5 mL benzaldehyde,n（30%H₂O₂）∶n（FeSO₄·7H₂O）=20∶1,and 1.0 mL 30%H₂O₂ were added and reacted at 0～2℃ for 6 h,the yield was 58.2%.The structure of the compound was confirmed by MS、（）¹H NMR and IR,and its antitumor activity was tested in vitro by SRB assays.The preliminary bioassay indicated that the compound was active against HL-60,BGC-823 and Bel-7402,especially BGC-823.更多还原