A novel class of small-molecule caspase-3 inhibitors prepared by multicomponent reactions
文献类型：期刊论文
| 作者 | Zhu, Qiuhua2,3; Gao, Lixin1; Chen, Zhipeng2; Zheng, Sichao2; Shu, Huafei2; Li, Jia1 ; Jiang, Huanfeng3; Liu, Shuwen2
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| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2012-08 |
| 卷号 | 54页码:232-238 |
| 关键词 | Caspase-3 inhibitor Dihydropyrrole Multicomponent reaction Synthesis |
| ISSN号 | 0223-5234 |
| DOI | 10.1016/j.ejmech.2012.05.001 |
| 文献子类 | Article |
| 英文摘要 | A series of tetra- and pentasubstituted polyfunctional dihydropyrroles 5 and 6 were synthesized via practical multicomponent reactions (MCRs) for research on their structure activity relationship as caspase-3 inhibitors. Among 39 compounds evaluated, 14 of them exhibited inhibition against caspase-3 with IC50 ranging from 5 to 20 mu M. The inhibitory activities of 5 and 6 depend on the nature of substituents on different positions. 5 and 6 possess a different scaffold from those previously reported and are the first caspase-3 inhibitors prepared via MCRs. The most active compounds 5k (IC50 = 5.27 mu M) could therefore be used as a lead for the development of highly potent caspase-3 inhibitors as drug candidates for therapeutic agents by taking advantage of MCRs. (C) 2012 Elsevier Masson SAS. All rights reserved. |
| WOS关键词 | PARTITION-COEFFICIENTS ; SULFONAMIDE ANALOGS ; DRUG DISCOVERY ; CELL-DEATH ; APOPTOSIS ; POTENT ; TETRAHYDROPYRIMIDINES ; SOLUBILITY ; MECHANISMS ; CANCER |
| 资助项目 | National Natural Foundation of China[U0832001] ; National Basic Research Program of China (973 Program)[2011CB808603] ; Guangdong Natural Science Foundation[10351086000000] ; Guangdong Science and Technology Project[2008B060600066] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000307920600024 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277994]  |
| 专题 | 国家新药筛选中心 药物安全性评价中心 |
| 通讯作者 | Liu, Shuwen |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai Inst Biol Sci, Chinese Natl Ctr Drug Screening, Shanghai 201203, Peoples R China 2.So Med Univ, Sch Pharmaceut Sci, Guangzhou 510515, Guangdong, Peoples R China; 3.S China Univ Technol, Sch Chem & Chem Engn, Guangzhou 510640, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Zhu, Qiuhua,Gao, Lixin,Chen, Zhipeng,et al. A novel class of small-molecule caspase-3 inhibitors prepared by multicomponent reactions[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2012,54:232-238. |
| APA | Zhu, Qiuhua.,Gao, Lixin.,Chen, Zhipeng.,Zheng, Sichao.,Shu, Huafei.,...&Liu, Shuwen.(2012).A novel class of small-molecule caspase-3 inhibitors prepared by multicomponent reactions.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,54,232-238. |
| MLA | Zhu, Qiuhua,et al."A novel class of small-molecule caspase-3 inhibitors prepared by multicomponent reactions".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 54(2012):232-238. |
入库方式： OAI收割
来源：上海药物研究所
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