Synthesis and HIV-1 integrase inhibition activity of some N-arylindoles
文献类型：期刊论文
| 作者 | Xu H[*]1; Liu WQ2; Fan LL1; Chen Y1; Yang LM2; Lv L1; Zheng YT[*]2 |
| 刊名 | CHEMICAL & PHARMACEUTICAL BULLETIN
 |
| 出版日期 | 2008 |
| 卷号 | 56期号:5页码:720-722 |
| 关键词 | N-arylindole anti-human immunodeficiency virus type 1 integrase inhibitor synthesis |
| ISSN号 | 0009-2363 |
| 通讯作者 | orgxuhui@nwsuaf.edu.cn ; zhengyt@mail.kiz.ac.cn |
| 合作状况 | 其它 |
| 英文摘要 | Eight simple N-arylindoles were designed, synthesized and evaluated as human immunodeficiency virus (HIV)-1 integrase inhibitors in vitro for the first time. Among these compounds, 3b, 3e and 3g demonstrated significant anti-HIV-1 integrase activity. Especially 3b showed the highest anti-HIV-1 integrase activity with EC50 value of 7.88 mu g/ml and TI value of 24.61. Meantime, some structure-activity relationships were also observed and will provide a new lead for design and discovery of more potent N-arylindoles as HIV-1 integrase inhibitors. |
| 收录类别 | SCI |
| 资助信息 | This work has been supported by the program for New Century Excellent University Talents (NCET-06-0868), State Educa- tion Ministry of China, and the Science & Technology Research Plan in Shaanxi Province of China (No. 2006K01-G31-04). We also would like to acknowledge Key Scientific and Technological Projects of Yunnan province (2004NG12), National 973 project of China (2006CB504200), The Knowl- edge Innovation Program of CAS (KSCX1-YW-R-24). |
| 原文出处 | 200856720.pdf |
| 语种 | 英语 |
| 公开日期 | 2010-08-24 |
| 源URL | [http://159.226.149.42:8088/handle/152453/4639]  |
| 专题 | 昆明动物研究所_分子免疫药理学 昆明动物研究所_动物模型与人类重大疾病机理重点实验室 |
| 作者单位 | 1.Laboratory of Pharmaceutical Synthesis, College of Sciences, Northwest A&F University; Yangling 712100, China 2.Laboratory of Molecular Immunopharmacology, Key Laboratory of Animal Models and Human Diseases Mechanisms, Kunming Institute of Zoology, Chinese Academy of Sciences; Kunming 650223, China |
| 推荐引用方式 GB/T 7714 | Xu H[*],Liu WQ,Fan LL,et al. Synthesis and HIV-1 integrase inhibition activity of some N-arylindoles[J]. CHEMICAL & PHARMACEUTICAL BULLETIN,2008,56(5):720-722. |
| APA | Xu H[*].,Liu WQ.,Fan LL.,Chen Y.,Yang LM.,...&Zheng YT[*].(2008).Synthesis and HIV-1 integrase inhibition activity of some N-arylindoles.CHEMICAL & PHARMACEUTICAL BULLETIN,56(5),720-722. |
| MLA | Xu H[*],et al."Synthesis and HIV-1 integrase inhibition activity of some N-arylindoles".CHEMICAL & PHARMACEUTICAL BULLETIN 56.5(2008):720-722. |
入库方式： OAI收割
来源：昆明动物研究所
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