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| 磺胺类黄酮衍生物20S蛋白酶体抑制剂的设计、合成与活性评价 | |
| 引用本文： | 杨冠宇,孙琦,王超,梁磊,许凤荣,牛彦,徐萍. 磺胺类黄酮衍生物20S蛋白酶体抑制剂的设计、合成与活性评价[J]. 中国药学, 2014, 23(9): 626-630. DOI: 10.5246/jcps.2014.09.080 |
| 作者姓名： | 杨冠宇 孙琦 王超 梁磊 许凤荣 牛彦 徐萍 |
| 作者单位： | 北京大学医学部药学院药物化学系,北京100191 |
| 基金项目： | The National Natural Science Foundation of China（Grant No.21202003）; the National Basic Research Program of China（Grant No.2012CB518000）; the Specialized Research Fund for the Doctoral Program of Higher Education of China（Grant No.20120001110010） |
| 摘 要： | 本文通过计算机辅助设计,设计并合成了一系列磺胺类黄酮衍生物作为非共价20S蛋白酶体抑制剂,并对其生物活性进行了测试。与先导化合物相比（β5亚基的IC50值为14.0μM）,化合物仅表现出局部的改善,但仍可作为一类潜在的20S蛋白酶体抑制剂。 |
| 关 键 词： | 磺胺类黄酮衍生物 非共价抑制剂 计算机辅助设计 20S蛋白酶体抑制剂 选择性 |
| 收稿时间： | 2014-04-15 |
Design,synthesis and biological evaluation of sulfonamide flavone derivatives as potential 20S proteasome inhibitors |
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| Guanyu Yang,Qi Sun,Chao Wang,Lei Liang,Fengrong Xu,Yan Niu,Ping Xu. Design,synthesis and biological evaluation of sulfonamide flavone derivatives as potential 20S proteasome inhibitors[J]. Journal of Chinese Pharmaceutical Sciences, 2014, 23(9): 626-630. DOI: 10.5246/jcps.2014.09.080 | |
| Authors: | Guanyu Yang Qi Sun Chao Wang Lei Liang Fengrong Xu Yan Niu Ping Xu |
| Affiliation: | ( Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China) |
| Abstract: | A new series of sulfonamide flavone derivatives are designed as non-covalent inhibitors of proteasome assisted with computer-aided drug design （CADD）. The desired compounds were synthesized successfully and the biological evaluation was subsequently accomplished. The results showed negligible improvement from our lead compound （IC50 for β5 subunit was 14.0 μM）. Thus, these flavone derivatives might be improved as potential 20S proteasome inhibitors. |
| Keywords: | Sulfonamide flavone derivatives Non-covalent inhibitor CADD 20S proteasome inhibitor Selectivity |
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