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| 4(3H)-喹唑啉酮衍生物的合成及体外抗肿瘤活性 | |
| 引用本文： | 曹胜利,蒋宇扬,冯玉萍,刘世英,高红核,张玫,万荣.4(3H)-喹唑啉酮衍生物的合成及体外抗肿瘤活性[J].药学学报,2007,42(7):741-746. |
| 作者姓名： | 曹胜利 蒋宇扬 冯玉萍 刘世英 高红核 张玫 万荣 |
| 作者单位： | 1. 首都师范大学,化学系,北京,100037 2. 清华大学,深圳研究生院,广东省化学生物学重点实验室,广东,深圳,518055;清华大学,化学系,生命有机磷化学与化学生物学教育部重点实验室,北京,100084 3. 清华大学,化学系,生命有机磷化学与化学生物学教育部重点实验室,北京,100084 |
| 基金项目： | 北京市自然科学基金;北京市教委科技发展计划项目 |
| 摘 要： | 将6-溴甲基-2-甲基-4(3H)-喹唑啉酮在无水磷酸钾存在下与二硫化碳以及不同的胺反应，合成了一系列具有二硫代氨基甲酸酯侧链的4(3H)-喹唑啉酮衍生物，其结构经ESI-MS，1H NMR，元素分析或HRMS所证实。采用MTT法测定了目标化合物8a~8q对人慢性髓性白血病K562细胞和人宫颈癌Hela细胞的体外抗肿瘤活性，结果表明化合物8q对K562和Hela细胞的体外生长具有显著的抑制作用，IC50值分别为0.5和12.0 μmol·L-1，因而可作为抗肿瘤药物研究的先导化合物。 |
| 关 键 词： | 4(3H)-喹唑啉酮 二硫代氨基甲酸酯 抗肿瘤活性 |
| 文章编号： | 0513-4870（2007）07-0741-06 |
| 收稿时间： | 2007-02-27 |
| 修稿时间： | 2007-02-27 |
Synthesis and in vitro antitumor activity of 4(3H)-quinazolinone derivatives bearing dithiocarbamate chains |
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| CAO Sheng-li,JIANG Yu-yang,FENG Yu-ping,LIU Shi-ying,GAO Hong-he,ZHANG Mei,WAN Rong.Synthesis and in vitro antitumor activity of 4(3H)-quinazolinone derivatives bearing dithiocarbamate chains[J].Acta Pharmaceutica Sinica,2007,42(7):741-746. | |
| Authors: | CAO Sheng-li JIANG Yu-yang FENG Yu-ping LIU Shi-ying GAO Hong-he ZHANG Mei WAN Rong |
| Institution: | 1. Department of Chemistry, Capital Normal University, Belting 100037, China ; 2. The Key Laboratory of Chemical Biology, Guangdong Province ; Graduate School at Shenzhen, Tsinghua University, Shenzhen 518055, China; 3. The Key Laboratory of Bioorganic Phosphorus Chemistry and Chemical Biology, Ministry of Education; Department of Chemistry, Tsinghua University, Beijing 100084, China |
| Abstract: | A series of 4(3H)-quinazolinone derivatives bearing dithiocarbamate side chains have been synthesized through the reaction of 6-bromomethyl-2-methyl-4(3H)-quinazolinone with CS2 and various amines in the presence of anhydrous K3PO4, and their structures were confirmed with ESI-MS, H NMR, elemental analysis or HRMS. The target compounds 8a -8q were tested for their in vitro antitumor activity against human myelogenous leukaemia K562 and human Hela cell lines by means of colorimetric MTT assay. Among the tested compounds, 8q exhibited in vitro inhibitory activity against K562 and Hela cells with IC50 values of 0.5 and 12.0 micromol x L(-01), respectively. Therefore, compound 8q is worthy to be a lead compound for the design and synthesis of new antitumor agents. |
| Keywords: | 4(3H)-quinazolinone dithiocarbamate antitumor activity |
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