论文部分内容阅读
目的设计合成eudistominU及其 6位甲氧基取代的衍生物并测试其抗肿瘤活性。方法以吲哚 3 甲醛和色胺或 5 甲氧基色胺为原料先缩合 ,再通过Pictet Spengler反应环合得到四氢 β 咔啉 ,然后用DDQ脱氢芳构化得到目标化合物。结果合成了eudistominU及其 6位甲氧基取代的衍生物 ,利用核磁共振、质谱进行了结构确认。结论合成了海洋生物碱eudistominU及其 6位甲氧基取代的衍生物 ,初步体外抗肿瘤试验结果表明两者均具有较强的抗肿瘤活性
Objective To design and synthesize eudistominU and its 6-methoxy-substituted derivatives and test their anti-tumor activity. Methods The hydrazine 3 and formaldehyde or 5-methoxy tryptamine were used as the raw material for the first condensation, followed by the Pictet Spengler reaction for cyclization to give tetrahydro-β-porphyrin, and then dehydroaromatization with DDQ to obtain the target compound. Results EudistominU and its 6-methoxy-substituted derivatives were synthesized and confirmed by NMR and MS. Conclusion The marine alkaloid eudistominU and its methoxy substituted derivatives were synthesized. The preliminary in vitro anti-tumor experiments showed that both have strong anti-tumor activity.