Synthesis and biological evaluation of 5-fluoroquinolone-3-carboxylic acids as potential HIV-1 integrase inhibitors
文献类型：期刊论文
| 作者 | He QQ1; Zhang X2,3; Yang LM2; Zheng YT2; Chen F[*]1 |
| 刊名 | JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
 |
| 出版日期 | 2013 |
| 卷号 | 28期号:4页码:671-676 |
| 关键词 | HIV-1 integrase inhibitor 5-fluoroquinolone-3-carboxylic acids anti-HIV activity metal chelating structure-activity relationship |
| 通讯作者 | rfchen@fudan.edu.cn |
| 合作状况 | 其它 |
| 英文摘要 | A series of new quinolone-3-carboxylic acids as HIV-1 integrase inhibitors featuring a fluorine atom at C-5 position were synthesized and evaluated for their antiviral activity in C8166 cell culture. These newly synthesized compounds showed anti-HIV activity against wild-type virus with an EC50 value ranging from 29.85 to 0.032 mu M. The most active compound 4e exhibited activity against wild-type virus and the mutant virus A17 with an EC50 value of 0.032 and 0.082 mu M, respectively. Preliminary structure-activity relationship of these 5-fluoroquinolone-3-carboxylic acids was also investigated. |
| 收录类别 | SCI |
| 资助信息 | The work was also supported in part by grants from the National Natural Science Foundation of China (20872018), from Chinese Academy of Sciences (KSCX2-YW-R-185), from the Eleventh Five- Year Key Scientific and Technological Program of China (2009ZX09501-029), and from National Basic Research Program of China (2009CB5223006). |
| 语种 | 英语 |
| WOS记录号 | WOS:000321693400003 |
| 公开日期 | 2013-08-27 |
| 源URL | [http://159.226.149.42:8088/handle/152453/7592]  |
| 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.Department of Chemistry, Fudan University, Shanghai, P R China 2.Key Laboratory of Animal Models and Human Disease Mechanisms of Chinese Academy of Sciences & Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, P R China 3.Faculty of Pharmacy, Kunming Medical University, Kunming, P R China |
| 推荐引用方式 GB/T 7714 | He QQ,Zhang X,Yang LM,et al. Synthesis and biological evaluation of 5-fluoroquinolone-3-carboxylic acids as potential HIV-1 integrase inhibitors[J]. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY,2013,28(4):671-676. |
| APA | He QQ,Zhang X,Yang LM,Zheng YT,&Chen F[*].(2013).Synthesis and biological evaluation of 5-fluoroquinolone-3-carboxylic acids as potential HIV-1 integrase inhibitors.JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY,28(4),671-676. |
| MLA | He QQ,et al."Synthesis and biological evaluation of 5-fluoroquinolone-3-carboxylic acids as potential HIV-1 integrase inhibitors".JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY 28.4(2013):671-676. |
入库方式： OAI收割
来源：昆明动物研究所
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