| 新型查尔酮类化合物的合成及其生物活性研究 |
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| 引用本文： | 廖头根,汪秋安,方伟琴,朱华结.新型查尔酮类化合物的合成及其生物活性研究[J].有机化学,2006,26(5):685-689. |
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| 作者姓名： | 廖头根 汪秋安 方伟琴 朱华结 |
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| 作者单位： | 湖南大学化学化工学院 长沙410082(廖头根，汪秋安，方伟琴)，中国科学院昆明植物研究所植物化学与西部植物资源持续利用国家重点实验室 昆明650204(朱华结) |
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| 基金项目： | 中科院昆明植物化学与西部植物资源持续利用国家重点实验室开放基金(2004年)资助项目. |
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| 摘 要： | 以3,5-二羟基苯甲酸为原料, 分别经酯化、甲氧甲基保护或甲基化、酰肼化、氧化、醛酮缩合、脱保护基、O-法呢基化或O-异戊烯基化等步骤, 以5.6%～46%的总收率合成了8个未见文献报道的查尔酮类化合物1a～1h, 产物通过1H NMR, 13C NMR, IR, MS进行了结构确证. 对所合成的目标化合物在3个标准活性筛选模型中进行了生物活性试验, 结果表明化合物1b在组织蛋白酶B (CAT-B)模型、化合物1e在细胞分离周期基因25表达的蛋白磷酸酶(CDC25)模型中表现出良好的活性.
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| 关 键 词： | 羟基查尔酮 法呢氧基查尔酮 异戊烯氧基查尔酮 合成 生物活性 |
| 收稿时间： | 07 21 2005 12:00AM |
| 修稿时间： | 11 2 2005 12:00AM |
Studies on the Synthesis of Novel Chalcone and Biological Activity |
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| LIAO Tou-Gen,WANG Qiu-An,FANG Wei-Qin,ZHU Hua-Jie.Studies on the Synthesis of Novel Chalcone and Biological Activity[J].Chinese Journal of Organic Chemistry,2006,26(5):685-689. |
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| Authors: | LIAO Tou-Gen WANG Qiu-An FANG Wei-Qin ZHU Hua-Jie |
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| Affiliation: | a College of Chemical and Chemistry Engineering, Hunan University, Changsha 410082;b State Key Laboratory of Photochemistry and Plant Resource in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650204 |
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| Abstract: | Eight novel chalcone compounds 1a-1h were synthesized by esterification, methoxymethyl protection or methylation, hydrazidation, oxidation, aldol condensation, deprotection, O-farnesylation or O-prenylation respectively using 3,5-dihydroxybenzoic acid as starting material in overall yields of 5.6%-46%. Their structures were confirmed by ^1H NMR, ^13C NMR, IR and MS spectra. Target compounds were screened with three international standard models for biological activity. Results showed that lb against model CAT-B and lc against model CDC25 possessed the good inhibition activity. |
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| Keywords: | hydroxylated chalcone farnesyloxy chalcone prenyloxy chalcone synthesis biological activity |
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