抗炎药物喜树碱的衍生化修饰

The modifier of anti-cancer camptothecin derivatives

目的为了增强喜树碱溶解性和提高它的抗肿瘤活性。方法采用了新颖的由喜树碱合成7-乙基喜树碱的路径,在此基础上利用阿司匹林对其20S-羟基酯化,并利用核磁共振仪、高分辨质谱、傅立叶变换红外光谱等对合成的产物跟踪表征。结果缩短了反应时间,提高了反应产率,可以达到较好修饰效果,确定了目标产物反应的最佳条件。结论两种修饰方式的协同作用可以有效的解决天然喜树碱溶解性差,母体毒副作用大的缺点。

Aim To improve the solubility and anti-tumor activity of camptothecin.Method A new synthesis path of conversion of camptothecin to 7-ethylcamptothecin was used,then aspirin modifier 7-ethylcamptothecin was used,by means of ^1HNMR,MS,FT-IR analysis.Results The reaction time has been greatly shortened and the yield of products has been improved.Optimized and improved reaction condition has been adopted.Conclusion Two modified form of synergy can effectively solve the poor solubility of camptothecin and the mother of the shortlomings of the side effects.