菲啶/苯骈菲啶衍生物抗肿瘤活性研究进展  

Progress on Antitumor Activity of Phenanthridine/benzo[c]phenanthridine Derivatives

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作  者:万明慧 李蔷 周宇涵[2] 宋伟国 

机构地区:[1]潍坊医学院,山东潍坊251053 [2]大连理工大学制药科学与技术学院,精细化工国家重点实验室,辽宁大连116024

出  处:《中国医药工业杂志》2018年第3期273-283,共11页Chinese Journal of Pharmaceuticals

摘  要:菲啶/苯骈菲啶衍生物是一类含氮杂环化合物,由于在抗肿瘤、抗血管生成、抗血小板、抗病毒和抗真菌等方面均表现出较好的生物活性而备受关注。本文按其主要作用靶点,如拓扑异构酶、微管蛋白、端粒酶等,综述了近年来菲啶/苯骈菲啶衍生物在抗肿瘤方面的研究进展。希望通过总结构效关系,探寻发现靶向性、高选择性、高效低毒的菲啶类抗肿瘤药物的结构规律,为进一步研究开发抗肿瘤药物提供帮助。Phenanthridine/benzo [c] phenanthridine are a series of heterocyclic compounds, which have received much attention and are used as antitumor, anti-angiogenesis, antiplatelet, antiviral and anti-fungal agents. This review focused on the recent progress on the antiturnor activity of natural and synthetic phenanthridine/benzo Eel -phenanthridines derivatives, including their inhibition on topoisomerase I /II, tubulin, telomerase, etc. Phenanthridines/benzo [el phenanthridines with high selectivity, targeting, high efficiency and low toxicity will be found through structure-activity relationship study, which will provide new sights for investigation of anti-tumor drugs.

关 键 词:菲啶衍生物 抗肿瘤活性 靶点 

分 类 号:R979.1[医药卫生—药品] O626[医药卫生—药学]

 

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