【摘 要】
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目的设计并全合成7-芳杂环高喜树碱衍生物并测试抗肿瘤活性。方法首先合成关键中间体5-乙基-5-羟基-4,5,8,9-四氢氧杂环庚三烯并[3,4-f]中氮茚-3,7,11(1H)-三酮,经Frilander
【机 构】
：
第二军医大学药学院,第二军医大学药学院,第二军医大学药学院,第二军医大学药学院,第二军医大学药学院,第二军医大学药学院,第二军医大学药学院,第二军医大学药学院,第二军医大学药学院 上海200433,上
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目的设计并全合成7-芳杂环高喜树碱衍生物并测试抗肿瘤活性。方法首先合成关键中间体5-乙基-5-羟基-4,5,8,9-四氢氧杂环庚三烯并[3,4-f]中氮茚-3,7,11(1H)-三酮,经Frilander反应得到7-氯甲基-10-甲基高喜树碱,然后与芳杂环生成目标产物。结果与结论合成了3个新化合物,化合物的结构经1H-NMR、FAB-MS谱确证,体外抗肿瘤活性测试结果显示化合物7和8c对肿瘤细胞A549、LOVO和MCF-7具有良好的抗肿瘤活性,优于拓扑替康。
Objective To design and synthesize 7-arylheterocyclic camptothecin derivatives and test their anti-tumor activity. Methods The key intermediate 5-ethyl-5-hydroxy-4,5,8,9-tetrahydrooxepino [3,4-f] indolizine-3,7,11 ) -trione to give 7-chloromethyl-10-methylhomocamptothecin via Frilander reaction, which is then coupled with an aromatic heterocycle to form the desired product. RESULTS AND CONCLUSIONS Three novel compounds were synthesized. The structures of the compounds were confirmed by 1H-NMR and FAB-MS. The antitumor activity in vitro showed that compounds 7 and 8c had good antitumor activity against tumor cells A549, LOVO and MCF-7 Activity, better than topotecan.
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