| 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 |
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| 引用本文： | 董肖椿,闻韧,郑剑斌. 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[J]. 药学学报, 2004, 39(4): 259-262 |
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| 作者姓名： | 董肖椿 闻韧 郑剑斌 |
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| 作者单位： | 复旦大学,药学院,药物化学教研室,上海,200032 |
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| 基金项目： | 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) |
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| 摘 要： | 目的设计合成eudistomin U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eudistomin U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eudistomin U及其一系列衍生物,初步体外抗肿瘤试验结果表明它们均具有一定的抗肿瘤活性。
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| 关 键 词： | 合成 抗肿瘤 eudistomin U 衍生物 |
| 收稿时间： | 2003-04-01 |
Synthesis of 1-indole substituted β-carboline alkaloid and its derivatives and evaluation of their preliminary antitumor activities |
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| DONG Xiao-chun,WEN Ren ,ZHENG Jian-bin. Synthesis of 1-indole substituted β-carboline alkaloid and its derivatives and evaluation of their preliminary antitumor activities[J]. Acta pharmaceutica Sinica, 2004, 39(4): 259-262 |
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| Authors: | DONG Xiao-chun WEN Ren ZHENG Jian-bin |
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| Affiliation: | Department of Medicinal Chemistry, College of Pharmacy, Fudan University, Shanghai 200032, China. |
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| Abstract: | AIM: To synthesize eudistomin U and its 6-OCH3/Br derivatives and 5'-Br derivatives as antitumor agents. METHODS: Using tryptamine and indole-3-aldehyde as starting materials, through condensation, Pictet-Spengler cyclization and dehydrogenation three steps, the alkaloids and its derivatives were prepared. RESULTS: The structures of the compounds were determined by 1HNMR, MS and HRMS. Antitumor activity in vitro was tested. CONCLUSION: Eudistomin U and its derivatives were synthesized. The results showed that they all showed antitumor activities against mouse P388 strain. |
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| Keywords: | synthesis eudistomin U antitumor derivatives |
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