苯并啡啶生物碱衍生物的设计合成及其活性研究

来源 :中国化学会全国第十一届有机合成化学学术研讨会 | 被引量 : 0次 | 上传用户：jakynum1

【摘要】

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【作者】

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孔石林戴求资李典鹏苏桂发潘成学

【机构】

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广西师范大学化学与药学学院药用资源化学与药物分子工程国家重点实验室培育基地桂林541004 广

【出处】

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中国化学会全国第十一届有机合成化学学术研讨会

【发表日期】

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2014年5期

【关键词】

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苯并啡啶天然产物结构改造抗肿瘤活性

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　　论文摘要苯并啡啶类生物碱(benzo [c]phenanthridine alkaloids)是一类四环异喹啉生物碱(Fig.1)，具有抗肿瘤、抗病毒、抗炎及抗菌等活性[1-2]，一些苯并啡啶类生物碱如两面针碱(Nitidine)、花椒宁碱(Fagaronine)等的抗肿瘤作用在临床上已在一定范围内使用，但由于其高毒性及水溶性差等原因，极大地限制了它们在临床上的广泛应用.因此，针对苯并啡啶类生物碱及其衍生物的合成方法及其生物活性研究，近年来一直受到广泛关注[3-5].考虑到苯并啡啶的四环骨架中氢键受体和氢键供体之和仅为1个，在其骨架中适当增加它们的数目，将有利于提高其类药性，优化其理化性质；另外考虑到这类生物碱的主要作用靶点为DNA及拓扑异构酶等，在其环系中引入嘧啶等杂环，很可能有利于增强其与相关靶点的相互作用，获得活性更好的衍生物.

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苯并啡啶生物碱衍生物的设计合成及其活性研究

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