Synthesis and biological evaluation of N-acetyl-beta-aryl-1,2-didehydroethylamines as new HIV-1 RT inhibitors in vitro
文献类型：期刊论文
| 作者 | Cheng P1,4; Jiang ZY1,3; Wang RR2; Zhang XM1,3; Wang Q2; Zheng YT[*]2; Zhou J1,3; Chen JJ[*]1,3 |
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2007 |
| 卷号 | 17期号:16页码:4476-4480 |
| 关键词 | N-acetyl-beta-aryl-1,2-didehydroethylamine beta-aryl-nitroolefin NNRTIs anti-HIV-1 RT activity |
| ISSN号 | 0960-894X |
| 通讯作者 | chenjj@mail.kib.ac.cn |
| 合作状况 | 其它 |
| 英文摘要 | A variety of N-acetyl-o-aryl-1,2-didehydroethylamines were synthesized by direct reduction-acetylation of beta-aryl-nitroolefins and assayed as HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) for the first time. Compound 7a exhibited a TI value of > 13.2 with CC50 value of > 0.787 mM in C8166 cells. This structure-activity relationship (SAR) study provided a new lead for design and discovery of more potent and selective analogues act as NNRTIs. |
| 收录类别 | SCI |
| 资助信息 | The work was partly supported by the 863 Program, Ministry of Science and Technology, PR Chi- na (2003AA2Z3512). |
| 原文出处 | 2007174476.pdf |
| 语种 | 英语 |
| 公开日期 | 2010-08-24 |
| 源URL | [http://159.226.149.42:8088/handle/152453/4591]  |
| 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.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.The Joint-Laboratory of Antiviral Natural Medicines, Kunming Branch, The Chinese Academy of Sciences, Kunming, Yunnan 650204, PR China 4.Graduate School of the Chinese Academy of Sciences, Beijing 100039, PR China |
| 推荐引用方式 GB/T 7714 | Cheng P,Jiang ZY,Wang RR,et al. Synthesis and biological evaluation of N-acetyl-beta-aryl-1,2-didehydroethylamines as new HIV-1 RT inhibitors in vitro[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2007,17(16):4476-4480. |
| APA | Cheng P.,Jiang ZY.,Wang RR.,Zhang XM.,Wang Q.,...&Chen JJ[*].(2007).Synthesis and biological evaluation of N-acetyl-beta-aryl-1,2-didehydroethylamines as new HIV-1 RT inhibitors in vitro.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,17(16),4476-4480. |
| MLA | Cheng P,et al."Synthesis and biological evaluation of N-acetyl-beta-aryl-1,2-didehydroethylamines as new HIV-1 RT inhibitors in vitro".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 17.16(2007):4476-4480. |
入库方式： OAI收割
来源：昆明动物研究所
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