1-吲哚基取代β-咔啉生物碱及其衍生物的合成和初步抗肿瘤活性  

Synthesis of 1-indole substituted β-carboline alkaloid and its derivatives and evaluation of their preliminary antitumor activities

作　　者：董肖椿[1] 闻韧[1] 郑剑斌[1] 

机构地区：[1]复旦大学药学院药物化学教研室,上海200032

出　　处：《药学学报》2004年第4期259-262,共4页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金资助项目 ( 2 98- 72 0 2 9);国际合作项目 ( 2 0 0 1 0 1 40 4 1 7)

摘　　要：目的　设计合成eudistominU及其 6位甲氧基 溴取代衍生物和 5′位溴取代衍生物并测试其抗肿瘤活性。方法　以吲哚 3 甲醛或 5 溴 吲哚 3 甲醛和色胺或取代色胺为原料先缩合 ,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 溴取代衍生物和 5′位溴取代衍生物 ,利用核磁共振、质谱、高分辨质谱确认结构。结论　合成了海洋生物碱eudistominU及其一系列衍生物 。AimTo synthesize eudistomin U and its 6-OCH 3/Br derivatives and 5′-Br derivati ves as antitumor agents. MethodsUsing tryptamine and indole-3-aldehyde as starting materials, through condensa tion, Pictet-Spengler cyclization and dehydrogenation three steps, the alkaloid s and its derivatives were prepared. ResultsThe structures of the compounds were determined by 1HNMR , MS and HRMS. Antitumor activity in vitro was tested. ConclusionEudistomin U and its derivatives were synthesized. The results showed that they all showed antitumor activities against mouse P388 strain.

关 键 词：1—吲哚基 β—咔啉生物碱 衍生物合成 抗肿瘤活性 

分 类 号：R979.1[医药卫生—药品]