Synthesis of New 2-(N-Arylsulfonylindol-3-yl)-3-aryl-1,3-thiazolidin-4-ones as HIV-1 Inhibitors In Vitro
文献类型：期刊论文
| 作者 | Yang RG1; Yang LM2; Ke YZ1; Huang N2,3; Zhang R1; Zheng YT[*]2; Xu H[*]1 |
| 刊名 | LETTERS IN DRUG DESIGN & DISCOVERY
 |
| 出版日期 | 2012 |
| 卷号 | 9期号:4页码:415-420 |
| 关键词 | 2-(N-Arylsulfonylindol-3-yl)-3-aryl-1,3-thiazolidin-4-ones Acquired immunodeficiency syndrome Human immunodeficiency virus-1 AIDS |
| 通讯作者 | orgxuhui@nwsuaf.edu.cn |
| 合作状况 | 其它 |
| 英文摘要 | Twenty-one 2-(N-arylsulfonylindol-3-yl)-3-aryl-1,3-thiazolidin-4-ones (4a-u) were synthesized and evaluated as HIV-1 inhibitors in vitro. Among all compounds, compounds 4n and 4p displayed the potent anti-HIV-1 activities with EC50 values of 3.48 and 8.61 mu g/mL, and TI values of 34.08 and > 23.22, respectively. It demonstrated that, to a series of 2-(N-arylsulfonyl-6-methylindol-3-yl)-3-aryl-1,3-thiazolidin-4-one derivatives, introduction of R-2 as 4-Cl and R-3 as H or 3-Cl could afford the more promising and potent compounds. |
| 收录类别 | SCI |
| 资助信息 | This work has been supported by the Special Funds of Central Colleges Basic Scientific Research Operating Expenses (QN2009045), and the Science & Technology Research Plan in Shaanxi province of China (2010K02-09- 3). We also would like to acknowledge the National Basic Research Program of China (2009CB522306), National Natural Science Foundation of China (81102483), Eleventh Five-Year Key Scientific and Technological Program of China (2009ZX09501-029) and the MRC AIDS Research Project and the NIH AIDS Research and Reference Reagent Program for providing cell lines and viruses. |
| 语种 | 英语 |
| 公开日期 | 2012-05-31 |
| 源URL | [http://159.226.149.42:8088/handle/152453/6957]  |
| 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 Design & Synthesis, College of Sciences, Northwest A&F University, Yangling, Shaanxi 712100, P. R. China 2.Key Laboratory of Animal Models and Human Diseases Mechanisms of Chinese Academy of Sciences and Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, Yunnan 650223, P. R. China 3.Graduate School of the Chinese Academy of Sciences, Beijing 100039, China |
| 推荐引用方式 GB/T 7714 | Yang RG,Yang LM,Ke YZ,et al. Synthesis of New 2-(N-Arylsulfonylindol-3-yl)-3-aryl-1,3-thiazolidin-4-ones as HIV-1 Inhibitors In Vitro[J]. LETTERS IN DRUG DESIGN & DISCOVERY,2012,9(4):415-420. |
| APA | Yang RG.,Yang LM.,Ke YZ.,Huang N.,Zhang R.,...&Xu H[*].(2012).Synthesis of New 2-(N-Arylsulfonylindol-3-yl)-3-aryl-1,3-thiazolidin-4-ones as HIV-1 Inhibitors In Vitro.LETTERS IN DRUG DESIGN & DISCOVERY,9(4),415-420. |
| MLA | Yang RG,et al."Synthesis of New 2-(N-Arylsulfonylindol-3-yl)-3-aryl-1,3-thiazolidin-4-ones as HIV-1 Inhibitors In Vitro".LETTERS IN DRUG DESIGN & DISCOVERY 9.4(2012):415-420. |
入库方式： OAI收割
来源：昆明动物研究所
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