Anti HIV-1 agents 5: Synthesis and anti-HIV-1 activity of some N-arylsulfonyl-3-acetylindoles in vitro
文献类型：期刊论文
| 作者 | Ran JQ1; Huang N2; Xu H[*]1; Yang LM2; Lv M[*]1; Zheng YT[*]2 |
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2010 |
| 卷号 | 20期号:12页码:3534-3536 |
| 关键词 | N-Arylsulfonyl-3-acetylindole Acquired immune-deficiency syndrome Human immunodeficiency virus-1 Inhibitor |
| ISSN号 | 0960-894X |
| 通讯作者 | orgxuhui@nwsuaf.edu.cn ; lvmin@nwsuaf.edu.cn ; zhengyt@mail.kiz.ac.cn |
| 合作状况 | 其它 |
| 英文摘要 | In continuation of our program aimed at the discovery and development of compounds with superior anti-human immunodeficiency virus type 1 (HIV-1) activity, 21N-arylsulfonyl-3-acetylindole analogs (2a-u) were synthesized and preliminarily evaluated as HIV-1 inhibitors in vitro. Among of all the analogs, several compounds exhibited significant anti-HIV-1 activity, especially N-phenylsulfonyl-3-acetyl-6-methylindole (2j) and N-(p-ethyl)phenylsulfonyl-3-acetyl-6-methylindole (2n) showed the most potent anti-HIV-1 activity with EC(50) values of 0.36 and 0.13 mu g/mL, and TI values of >555.55 and 791.85, respectively. It demonstrated that introduction of the acetyl group at the 3-position of N-arylsulfonyl-6-methylindoles could generally lead to the more potent analogs. |
| 收录类别 | 其他 |
| 资助信息 | This study was supported by National Science Foundation of China (NSFC 30870825, 30530270, 30670669 and 30770700). The author gratefully acknowledges the support of K.C. Wong Education Foundation, Hong Kong. |
| 原文出处 | 201020123534.pdf |
| 语种 | 英语 |
| 公开日期 | 2010-08-24 |
| 源URL | [http://159.226.149.42:8088/handle/152453/4693]  |
| 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 712100, 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 650223, China |
| 推荐引用方式 GB/T 7714 | Ran JQ,Huang N,Xu H[*],et al. Anti HIV-1 agents 5: Synthesis and anti-HIV-1 activity of some N-arylsulfonyl-3-acetylindoles in vitro[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2010,20(12):3534-3536. |
| APA | Ran JQ,Huang N,Xu H[*],Yang LM,Lv M[*],&Zheng YT[*].(2010).Anti HIV-1 agents 5: Synthesis and anti-HIV-1 activity of some N-arylsulfonyl-3-acetylindoles in vitro.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,20(12),3534-3536. |
| MLA | Ran JQ,et al."Anti HIV-1 agents 5: Synthesis and anti-HIV-1 activity of some N-arylsulfonyl-3-acetylindoles in vitro".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 20.12(2010):3534-3536. |
入库方式： OAI收割
来源：昆明动物研究所
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