| 6,7-二甲氧基-4-哌嗪喹唑啉缩氨基硫脲衍生物的合成及体外抗肿瘤活性研究 |
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| 引用本文： | 刘海彬,徐惠娟,吕萍,潘宁宁,李双奇.6,7-二甲氧基-4-哌嗪喹唑啉缩氨基硫脲衍生物的合成及体外抗肿瘤活性研究[J].化学学报,2012,70(5):674-678. |
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| 作者姓名： | 刘海彬 徐惠娟 吕萍 潘宁宁 李双奇 |
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| 作者单位： | 辽宁科技学院生物医药与化学工程学院,本溪,117004 |
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| 基金项目： | 辽宁省教育厅科研项目，辽宁省高等学校优秀人才支持计划，辽宁科技学院博士启动金 |
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| 摘 要： | 以4,5-二甲氧基-2-氨基苯甲酸和醋酸甲眯为起始原料,经环化、氯化、取代和缩合四步反应,设计、合成了六个未见文献报道的含有缩氨基硫脲的喹唑啉衍生物4a～4f,其结构用1H NMR,13C NMR,ESI-MS,IR及元素分析测试技术进行了表征.采用MTT法测试了化合物4a～4f对人胃癌SGC-7901、人口腔表皮样癌KB和人纤维肉瘤HT-1080的体外抗肿瘤活性.初步的测试结果表明,化合物4a和4f对HT1080表现出显著的抗肿瘤活性.
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| 关 键 词： | 喹唑啉 缩氨基硫脲 抗肿瘤活性 MTT法 |
Synthesis and in vitro Antitumor Activities of 6,7-Dimethoxy-4-piperazinquinazoline Thiosemicarbazone Derivatives |
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| Institution: | Liu,Haibin Xu,Huijuan Lü,Ping Pan,Ningning Li,Shuangqi(School of Biomedical & Chemical Engineering,Liaoning Institute of Science and Technology,Benxi 117004) |
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| Abstract: | Six new quinazoline derivatives 4a～4f bearing thiosemicabazone have been designed and synthesized by four step reactions of cyclization,chlorination,substitution and condensation using 2-amino-4,5-dimethoxybenzoic acid and methanimidamide acetate as starting materials.Their structures were confirmed by 1H NMR,13C NMR,ESI-MS,IR techniques and elemental analysis.The in vitro antitumor activities of compounds 4a～4f against SGC-7901(human gastric cancer),KB(human oral epidermoid cancer) and HT-1080(human fibrosarcoma) cell lines were tested using colorimetric MTT assay.The preliminary results indicated that compounds 4a and 4f showed significant antitumor activity against HT1080. |
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| Keywords: | quinazoline thiosemicarbazone antitumor activity MTT assay |
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