Synthesis and biological evaluation of novel amprenavir-based P1-substituted bi-aryl derivatives as ultra-potent HIV-1 protease inhibitors
文献类型：期刊论文
| 作者 | Yan, Jianwei2; Huang, Ning1; Li, Shukun2; Yang, Liu-Meng1; Xing, Weiqiang2; Zheng, Yong-Tang1; Hu, Youhong2
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2012-03-01 |
| 卷号 | 22期号:5页码:1976-1979 |
| 关键词 | HIV-1 protease inhibitors Amprenavir Darunavir biaryl compounds Docking study |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2012.01.037 |
| 文献子类 | Article |
| 英文摘要 | A series of P1-substituted biaryl amprenavir derivatives was designed and synthesized. These compounds were evaluated for enzyme inhibition and antiviral activity in vitro. Several compounds showed highly efficient antiviral activity with EC50 values down to 0.10 nM, which are more potent than marketed HIV-1 protease inhibitors. Docking study indicated that 12c has similar binding mode to amprenavir with full occupancy in P1. (C) 2012 Elsevier Ltd. All rights reserved. |
| WOS关键词 | STRUCTURE-BASED DESIGN ; TERTIARY-ALCOHOL ; INSULIN-RESISTANCE ; P2 LIGANDS ; VIRUS ; DISCOVERY ; LIPODYSTROPHY ; MORTALITY ; INFECTION ; INDINAVIR |
| 资助项目 | National Natural Science Foundation of China[30600775] ; National Natural Science Foundation of China[81001462] ; Eleventh Five-Year Key Scientific and Technological Program of China[2009ZX09501-029] ; CAS[KSCX2-YW-R-185] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000300451200028 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278176]  |
| 专题 | 药物化学研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 |
| 通讯作者 | Zheng, Yong-Tang |
| 作者单位 | 1.Chinese Acad Sci, Key Lab Anim Models & Human Dis Mech, Chinese Acad Sci & Yunnan Prov, Kunming Inst Zool, Kunming 650223, Yunnan, Peoples R China; 2.Chinese Acad Sci, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Yan, Jianwei,Huang, Ning,Li, Shukun,et al. Synthesis and biological evaluation of novel amprenavir-based P1-substituted bi-aryl derivatives as ultra-potent HIV-1 protease inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2012,22(5):1976-1979. |
| APA | Yan, Jianwei.,Huang, Ning.,Li, Shukun.,Yang, Liu-Meng.,Xing, Weiqiang.,...&Hu, Youhong.(2012).Synthesis and biological evaluation of novel amprenavir-based P1-substituted bi-aryl derivatives as ultra-potent HIV-1 protease inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,22(5),1976-1979. |
| MLA | Yan, Jianwei,et al."Synthesis and biological evaluation of novel amprenavir-based P1-substituted bi-aryl derivatives as ultra-potent HIV-1 protease inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 22.5(2012):1976-1979. |
入库方式： OAI收割
来源：上海药物研究所
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