| N-芳乙基异喹啉衍生物的合成及其抗肿瘤活性研究 |
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| 作者姓名： | Wang YX Zhao WL Bi CW Li YB Shao RG Song DQ |
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| 作者单位： | (中国医学科学院、北京协和医学院医药生物技术研究所, 北京 100050) |
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| 基金项目： | “十二五重大新药创制”科技重大专项资助项目(2012ZX09301002-001-017) |
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| 摘 要： | 本研究采用一种简便的新方法设计合成了一系列全新结构的N-芳乙基异喹啉衍生物, 并对其体外抗肿瘤活性进行了评价。其中化合物9a表现出较强的抗肿瘤活性, 对人肝癌HepG2和大肠癌HCT116细胞的IC50值分别为2.52和1.99 μg·mL–1。初步作用机制显示, 9a可以将HepG2细胞周期阻滞于S期, 使细胞增殖受阻, 达到抗肿瘤效果。
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| 关 键 词： | N-芳乙基异喹啉 抗肿瘤 构效关系 |
Synthesis and structure-activity relationship of N-(2-arylethyl) isoquinoline derivatives as anti-cancer agents |
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| Wang YX,Zhao WL,Bi CW,Li YB,Shao RG,Song DQ.Synthesis and structure-activity relationship of N-(2-arylethyl) isoquinoline derivatives as anti-cancer agents[J].Acta Pharmaceutica Sinica,2012,47(2):200-205. |
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| Authors: | Wang Yan-Xiang Zhao Wu-Li Bi Chong-Wen Li Yang-Biao Shao Rong-Guang Song Dan-Qing |
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| Institution: | Institute of Medicinal Biotechnology, China Academy of Medical Science and Peking Union Medical College, Beijing 100050, China. |
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| Abstract: | A series of novel N-(2-arylethyl) isoquinoline derivatives were designed, synthesized and evaluated for their anti-cancer activities. Among these analogs, compound 9a exhibited the potential anti-cancer activities on HepG2 and HCT116 cells with IC50 values of 2.52 and 1.99 μg·mL–1, respectively. Cell cycle was blocked at S phase of HepG2 cells treated with 9a by flow cytometry detection. Our results provided a basis for the development of a new series of anti-cancer candidates. |
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| Keywords: | N-(2-arylethyl) isoquinoline anti-cancer structure-activity relationship |
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