| Synthesis and biological evaluation of N-acetyl-beta-aryl-1,2-didehydroethylamines as new HIV-1 RT inhibitors in vitro | |
| Cheng P1,4; Jiang ZY1,3; Wang RR2; Zhang XM1,3; Wang Q2; Zheng YT*2; Zhou J1,3; Chen JJ*1,3; chenjj@mail.kib.ac.cn | |
| 2007 | |
| 发表期刊 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| ISSN | 0960-894X |
| 卷号 | 17期号:16页码:4476-4480 |
| 合作性质 | 其它 |
| 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. |
| 关键词 | Beta-aryl-nitroolefin N-acetyl-beta-aryl-1 Nnrtis 2-didehydroethylamine Anti-hiv-1 Rt Activity |
| 资助者 | The work was partly supported by the 863 Program, Ministry of Science and Technology, PR Chi- na (2003AA2Z3512). ; The work was partly supported by the 863 Program, Ministry of Science and Technology, PR Chi- na (2003AA2Z3512). ; The work was partly supported by the 863 Program, Ministry of Science and Technology, PR Chi- na (2003AA2Z3512). ; The work was partly supported by the 863 Program, Ministry of Science and Technology, PR Chi- na (2003AA2Z3512). |
| URL | 查看原文 |
| 收录类别 | SCI |
| 语种 | 英语 |
| 资助者 | The work was partly supported by the 863 Program, Ministry of Science and Technology, PR Chi- na (2003AA2Z3512). ; The work was partly supported by the 863 Program, Ministry of Science and Technology, PR Chi- na (2003AA2Z3512). ; The work was partly supported by the 863 Program, Ministry of Science and Technology, PR Chi- na (2003AA2Z3512). ; The work was partly supported by the 863 Program, Ministry of Science and Technology, PR Chi- na (2003AA2Z3512). |
| 文献类型 | 期刊论文 |
| 条目标识符 | http://ir.kiz.ac.cn/handle/152453/4591 |
| 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.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.,...&chenjj@mail.kib.ac.cn.(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. |
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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 | ||
| 2007174476.pdf（148KB） | 期刊论文 | 出版稿 | 开放获取 | CC BY-NC-SA | 请求全文 | |
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