Synthesis and biological evaluation of HQCAs with aryl or benzyl substituents on N-1 position as potential HIV-1 integrase inhibitors
文献类型：期刊论文
| 作者 | He QQ1; Zhang X2; Wu HQ1; Gu SX1; Ma XD1; Yang LM2; Zheng YT2; Chen FE[*]1,3 |
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2011 |
| 卷号 | 19期号:18页码:5553-5558 |
| 关键词 | HIV Integrase inhibitor Quinolone-3-carboxylic acids Two-metal chelating mechanism Structure-activity relationships |
| 通讯作者 | rfchen@fudan.edu.cn |
| 合作状况 | 其它 |
| 英文摘要 | A series of new 5-hydroxylquinolone-3-carboxylic acids (HQCAs) with various aryl or benzyl substituents on N-1 position were synthesized and evaluated for their anti-HIV activity in C8166 cell culture. Most of the target compounds displayed activity against wide-type HIV-1 in the low micromolar range in infected C8166 cells. The most active compound 5g exhibited activity against wild-type HIV-1 and HIV-1 mutant virus A17 with an EC(50) value of 3.17 and 17.88 mu M, respectively. The biological results and the docking study revealed that the substitution pattern on N-1 position of the quinolone core might contribute to physicochemical properties of HQCAs and resulted in great influence on their antiviral potency. |
| 收录类别 | SCI |
| 资助信息 | This project was funded by China Postdoctoral Science Founda- tion(20100470624). 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 |
| 公开日期 | 2011-09-23 |
| 源URL | [http://159.226.149.42:8088/handle/353002/6810]  |
| 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.Key Laboratory of Animal Models and Human Disease Mechanisms of Chinese Academy of Sciences and Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, PR China 3.Institute of Biomedical Science, Fudan University, Shanghai 200433, PR China |
| 推荐引用方式 GB/T 7714 | He QQ,Zhang X,Wu HQ,et al. Synthesis and biological evaluation of HQCAs with aryl or benzyl substituents on N-1 position as potential HIV-1 integrase inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2011,19(18):5553-5558. |
| APA | He QQ.,Zhang X.,Wu HQ.,Gu SX.,Ma XD.,...&Chen FE[*].(2011).Synthesis and biological evaluation of HQCAs with aryl or benzyl substituents on N-1 position as potential HIV-1 integrase inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY,19(18),5553-5558. |
| MLA | He QQ,et al."Synthesis and biological evaluation of HQCAs with aryl or benzyl substituents on N-1 position as potential HIV-1 integrase inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY 19.18(2011):5553-5558. |
入库方式： OAI收割
来源：昆明动物研究所
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