| 一种新型Hsp90抑制剂的合成及其抑制活性 |
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| 引用本文： | 张晓颖,张杰,李伟,王小龙.一种新型Hsp90抑制剂的合成及其抑制活性[J].合成化学,2011,19(5). |
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| 作者姓名： | 张晓颖 张杰 李伟 王小龙 |
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| 作者单位： | 南京中医药大学药学院,江苏南京,210029 |
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| 摘 要： | 对氨基苯甲酸经重氮化后再与2-氯乙酰乙酸乙酯反应制得(Z)-4-2-(1-氯-2-乙氧基-2-羰亚甲基)肼基]苯甲酸(1);1与二甲基环己二酮成环后再与对羟基环己胺完成酰胺化反应合成了一种新型Hsp90抑制剂——N-(4-羟基环己基)-4-1-(6,6-二甲基-4-氧-3-乙酰氧基-4,5,6,7-四氢吲唑)]苯甲酰胺(3),其结构经1HNMR表征。荧光偏振法研究结果表明3对Hsp90α具有明显的抑制活性。
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| 关 键 词： | Hsp90抑制剂 对氨基苯甲酸 环己二酮 荧光偏振法 抑制活性 合成 |
Synthesis of Novel Hsp90 Inhibotor and Its Inhibition |
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| ZHANG Xiao-ying,ZHANG Jie,LI Wei,WANG Xiao-long.Synthesis of Novel Hsp90 Inhibotor and Its Inhibition[J].Chinese Journal of Synthetic Chemistry,2011,19(5). |
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| Authors: | ZHANG Xiao-ying ZHANG Jie LI Wei WANG Xiao-long |
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| Institution: | ZHANG Xiao-ying,ZHANG Jie,LI Wei,WANG Xiao-long(Institute of Pharmacy,Nanjing University of Chinese Medicine,Nanjing 210029,China) |
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| Abstract: | (Z)-4-2-(1-chloro-2-ethoxy-2-oxoethylidene)hydrazinyl]benzoic acid(1) was prepared from p-aminobenzoic acid by diazotization,then reacted with ethyl 2-chloro-acetoacetate.A novel Hsp90 inhibotor,ethyl 1-{4-(4-hydroxycyclohexyl)carbamoyl]phenyl}-6,6-dimethyl-4-oxo-4,5,6,7-tetrahydro-1H-indazole-3-carboxylate(3),was synthesized by cyclization between 1 and 5,5-dimethyl-cyclohexane-1,3-dione,then amidation with p-hydroxyl-cyclohexylamine.The structure was characterized by 1H NMR.The result from fluorescence ... |
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| Keywords: | Hsp90 Inhibitor p-aminobenzoic acid cyclohexane-1 3-dione fluorescence polarization inhibition synthesis |
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