| 6-取代1-氮杂苯并蒽酮衍生物的合成及抗肿瘤活性研究 |
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| 引用本文： | 唐煌,王志宇,钟书明,覃江克.6-取代1-氮杂苯并蒽酮衍生物的合成及抗肿瘤活性研究[J].广西师范大学学报(自然科学版),2012,30(2):78-82. |
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| 作者姓名： | 唐煌 王志宇 钟书明 覃江克 |
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| 作者单位： | 广西师范大学药用资源化学与药物分子工程教育部重点实验室,广西桂林,541004 |
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| 基金项目： | 国家自然科学基金，广西师范大学博士启动基金 |
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| 摘 要： | 以DNA双螺旋结构为靶点,设计合成了一系列新的6-取代的氧化异阿朴菲生物碱衍生物3a～3e。所有化合物的结构均用ESI-MS,1HNMR和元素分析确认。运用紫外吸收光谱研究了氧化异阿朴菲生物碱衍生物与小牛胸腺DNA(ctDNA)的相互作用。用MTT法评价衍生物对HepG2、SGC-7901、SW480、786-O和NCI-H460 5种肿瘤细胞的毒性。光谱研究结果表明衍生物能与ctDNA发生嵌插结合作用,细胞毒性测试表明衍生物具有中等强度的抗肿瘤活性。
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| 关 键 词： | 氧化异阿朴菲衍生物 DNA 抗肿瘤 合成 |
Synthesis and Antitumor Activity of 6-Substituted 1-Azabenzanthrone |
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| TANG Huang
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WANG Zhi-yu
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ZHONG Shu-ming
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QIN Jiang-ke.Synthesis and Antitumor Activity of 6-Substituted 1-Azabenzanthrone[J].Journal of Guangxi Normal University(Natural Science Edition),2012,30(2):78-82. |
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| Authors: | TANG Huang WANG Zhi-yu ZHONG Shu-ming QIN Jiang-ke |
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| Institution: | (Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources,Ministry of Education ofChina,Guangxi Normal University,Guilin Guangxi 541004,China) |
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| Abstract: | A series of novel 6-Substituted 1-Azabenzanthrone derivatives 3a～3e had been synthesized based on double helix DNA.All the target compounds were characterized by ESI-MS,1H NMR and element analysis.The interaction of derivatives with calf thymus DNA was performed by UV spectra.The in vitro cytotoxicity of derivatives for five cell lines(HepG2,SGC-7901,SW480,786-O and NCI-H460) was evaluated using MTT method.The experimental results indicated that the derivatives could intercalate calf thymus DNA and showed moderate cytotoxicity against different tumor cell lines. |
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| Keywords: | oxoisoaporphine derivatives DNA antitumor synthesis |
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