| 6-氟-4-(N-芳基)胺基喹唑啉类化合物的微波合成及生物活性研究 |
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| 引用本文： | 张培权,宋宝安,杨松,金林红,胡德禹,刘刚,薛伟.6-氟-4-(N-芳基)胺基喹唑啉类化合物的微波合成及生物活性研究[J].有机化学,2006,26(9):1275-1278. |
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| 作者姓名： | 张培权 宋宝安 杨松 金林红 胡德禹 刘刚 薛伟 |
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| 作者单位： | 贵州大学精细化工研究开发中心,教育部绿色农药和农业生物工程重点实验室,贵阳,550025 |
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| 基金项目： | 国家自然科学基金(No.20562003)，2005年贵州省优秀青年科技人才(No.20050515)资助项目. |
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| 摘 要： | 经2-氨基-5-氟苯甲酸与甲酰胺闭环、氯化反应, 合成了6-氟-4-氯喹唑啉, 然后在微波辐射下与芳香胺反应, 合成了6个新的6-氟-4-(N-芳基)胺基喹唑啉类化合物. 新化合物经1H NMR, IR及元素分析证明其结构. 体外抑瘤试验证明化合物对前列腺癌细胞(PC3)、人胃癌细胞(BGC823)、人乳腺癌细胞(BCap-37)均无抑制活性. 经ERK的抗磷酸化活性免疫印迹试验证明化合物对小鼠成纤维细胞(NIH3T3)无抑制活性.
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| 关 键 词： | 喹唑啉 氟 合成 微波辐射 生物活性 |
| 收稿时间： | 09 13 2005 12:00AM |
| 修稿时间： | 03 9 2006 12:00AM |
Synthesis and Bioactivity of 6-Fluoro-4-(N-aryl)aminoquinazoline Compounds under Microwave Irradiation |
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| ZHANG Pei-Quan,SONG Bao-An,YANG Song,JIN Lin-Hong,HU De-Yu,LIU Gang,XUE Wei.Synthesis and Bioactivity of 6-Fluoro-4-(N-aryl)aminoquinazoline Compounds under Microwave Irradiation[J].Chinese Journal of Organic Chemistry,2006,26(9):1275-1278. |
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| Authors: | ZHANG Pei-Quan SONG Bao-An YANG Song JIN Lin-Hong HU De-Yu LIU Gang XUE Wei |
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| Institution: | Key Laboratory of Green Pesticide and Agriculture Bioengineering, Ministry of Education, Research and Development Centre for Fine Chemicals, Guizhou University, Guiyang 550025 |
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| Abstract: | Six new 6-fluoro-4-(N-aryl)aminoquinazoline compounds were synthesized, firstly by the cycli- zation reaction of 2-amino-5-fluorobenzoic acid with formamide and then chlorination to attain 4-chloro-6-fluoroquinazoline, finally the amination with arylamines under microwave irradiation. The struc- tures of the six new compounds were characterized by elemental analyses, IR and 1H NMR spectra. Bioac- tivity of the new compounds was tested. The results showed that the six new compounds had weak antican- cer activity to PC3, BGC823, BCap-37 and ERK phosphorylation in NIH3T3 cell induced by PDGF. |
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| Keywords: | qunazoline fluorine synthesis microwave irradiation bioactivity |
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