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, Pi; Jiang, Zhi-Yong; Wang, Rul-Rul; Zhang, Xue-Mel; Wang, Qian ; Zheng, Yong-Tang; Zhou, Jun; Chen, Ji-Jun
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2007-08-15 |
| 卷号 | 17期号:16页码:4476-4480 |
| 关键词 | Beta-aryl-nitroolefin N-acetyl-beta-aryl-1 Nnrtis 2-didehydroethylamine Anti-hiv-1 Rt Activity |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2007.06.008 |
| 文献子类 | Article |
| 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. (c) 2007 Elsevier Ltd. All rights reserved. |
| 学科主题 | Chemistry ; Medicinal ; Chemistry ; Organic |
| WOS关键词 | ALKALOIDS |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000248877800014 |
| 公开日期 | 2011-11-24 |
| 源URL | [http://ir.kib.ac.cn:8080/handle/151853/2045]  |
| 专题 | 昆明植物研究所_植物化学与西部植物资源持续利用国家重点实验室 |
| 作者单位 | 1.Chinese Acad Sci, Kunming Inst Zool, Key Lab Anim Models & Human Dis Mech, Lab Mol Immunopharmacol, Kunming 650223, Peoples R China 2.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resource W China, Kunming 650204, Peoples R China 3.Chinese Acad Sci, Joint Lab Antiviral Nat Med, Kunming 650204, Peoples R China 4.Chinese Acad Sci, Grad Sch, Beijing 100039, Peoples R China |
| 推荐引用方式 GB/T 7714 | Cheng, Pi,Jiang, Zhi-Yong,Wang, Rul-Rul,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, Pi.,Jiang, Zhi-Yong.,Wang, Rul-Rul.,Zhang, Xue-Mel.,Wang, Qian.,...&Chen, Ji-Jun.(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, Pi,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：昆明植物研究所
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