| 1-Aryl-tetrahydroisoquinoline analogs as active anti-HIV agents in vitro | |
| Cheng P1,3; Huang N2; Jiang ZY1; Zhang Q1,3; Zheng YT2; Chen JJ*1; Zhang XM1; Ma YB1; chenjj@mail.kib.ac.cn | |
| 2008 | |
| 发表期刊 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 卷号 | 18期号:7页码:2475–2478 |
| 合作性质 | 其它 |
| 摘要 | A series of 1-aryl-6,7-dihydroxyl(methoxy)-1,2,3,4-tetrahydroisoquinolines (compounds 1–36) were synthesized via Pictet– Spengler cyclization. All the synthesized compounds were assayed for activities against HIV-1IIIB in C8166 cell cultures by MTT method for the first time. The results of the anti-HIV screening revealed that 6,7-dihydroxytetrahydroisoquinolines possessed higher selective index than 6,7-dimethoxyl analogs due to the significantly decreased cytotoxicities. Compounds 6, 24, and 36 showed potent anti-HIV activities with EC50 values of 8.2, 4.6, and 5.3 lM respectively, and the cytotoxicities (CC50) of these three compounds were 784.3, 727.3, and 687.3 lM, which resulted in SI values larger than 95, 159, and 130 respectively. |
| 关键词 | 1-aryl-tetrahydroisoquinoline Anti-hiv Activity Pictet-spengler Cyclization |
| 收录类别 | SCI |
| 语种 | 英语 |
| 文献类型 | 期刊论文 |
| 条目标识符 | http://ir.kiz.ac.cn/handle/152453/6391 |
| 专题 | 科研部门_分子免疫药理学（郑永唐） 科研部门_动物模型与人类重大疾病机理重点实验室 |
| 通讯作者 | chenjj@mail.kib.ac.cn |
| 作者单位 | 1.State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, The Chinese Academy of Sciences, Kunming, Yunnan 650204, PR China 2.Laboratory of Molecular Immunopharmacology, Key Laboratory of Animal Models and Human Diseases Mechanisms, Kunming Institute of Zoology, The Chinese Academy of Sciences, Kunming, Yunnan 650223, PR China 3.Graduate School of the Chinese Academy of Sciences, Beijing 100039, PR China |
| 推荐引用方式 GB/T 7714 | Cheng P,Huang N,Jiang ZY,et al. 1-Aryl-tetrahydroisoquinoline analogs as active anti-HIV agents in vitro[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2008,18(7):2475–2478. |
| APA | Cheng P.,Huang N.,Jiang ZY.,Zhang Q.,Zheng YT.,...&chenjj@mail.kib.ac.cn.(2008).1-Aryl-tetrahydroisoquinoline analogs as active anti-HIV agents in vitro.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,18(7),2475–2478. |
| MLA | Cheng P,et al."1-Aryl-tetrahydroisoquinoline analogs as active anti-HIV agents in vitro".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 18.7(2008):2475–2478. |
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| 文件名称/大小 | 文献类型 | 版本类型 | 开放类型 | 使用许可 | ||
| 2010111018.pdf（124KB） | 期刊论文 | 出版稿 | 开放获取 | CC BY-NC-SA | 请求全文 | |
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