Structural modifications of quinolone-3-carboxylic acids with anti-HIV activity
文献类型：期刊论文
| 作者 | He QQ1; Gu SX1; Liu J2; Wu HQ1; Zhang X3; Yang LM3; Zheng YT3; Chen FE[*]1,4 |
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2011 |
| 卷号 | 19期号:16页码:5039-5045 |
| 关键词 | HIV Integrase inhibitor Quinolone-3-carboxylic acids Two-metal chelating mechanism |
| 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 featuring a hydroxyl group at C-5 position were synthesized and evaluated for their in vitro activity against HIV in C8166 cell culture. All the compounds showed anti-HIV-1 activity with low micromolar to submicromolar EC(50) values. The most active compound 2k exhibited activity against wild-type HIV-1 with an EC(50) value of 0.13 mu M. Preliminary structure-activity relationship of the newly synthesized quinolone analogues was also investigated. Further docking study revealed that the anti-HIV activity of these compounds might involve a two-metal chelating mechanism. |
| 收录类别 | SCI |
| 资助信息 | This project was funded by China Postdoctoral Science Founda- tion (20100470625). The work was also supported in part by grant 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 Re- search Program of China (2009CB5223006). |
| 语种 | 英语 |
| 公开日期 | 2011-08-26 |
| 源URL | [http://159.226.149.42:8088/handle/353002/6711]  |
| 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 200433, PR China 2.Department of Medicinal Chemistry, School of Pharmacy, Second Millitary Medical University, Shanghai 200433, PR China 3.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 650223, PR China 4.Institute of Biomedical Science, Fudan University, Shanghai 200433, PR China |
| 推荐引用方式 GB/T 7714 | He QQ,Gu SX,Liu J,et al. Structural modifications of quinolone-3-carboxylic acids with anti-HIV activity[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2011,19(16):5039-5045. |
| APA | He QQ.,Gu SX.,Liu J.,Wu HQ.,Zhang X.,...&Chen FE[*].(2011).Structural modifications of quinolone-3-carboxylic acids with anti-HIV activity.BIOORGANIC & MEDICINAL CHEMISTRY,19(16),5039-5045. |
| MLA | He QQ,et al."Structural modifications of quinolone-3-carboxylic acids with anti-HIV activity".BIOORGANIC & MEDICINAL CHEMISTRY 19.16(2011):5039-5045. |
入库方式： OAI收割
来源：昆明动物研究所
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