Structural modifications of 5,6-dihydroxypyrimidines with anti-HIV activity
文献类型：期刊论文
| 作者 | Guo, Di-Liang1,3; Zhang, Xing-Jie2; Wang, Rui-Rui2; Zhou, Yu1 ; Li, Zeng1; Xu, Jin-Yi3; Chen, Kai-Xian1,3; Zheng, Yong-Tang2; Liu, Hong1,3
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2012-12-01 |
| 卷号 | 22期号:23页码:7114-7118 |
| 关键词 | Dihydroxypyrimidine Synthesis HIV Integrase inhibitor Docking study |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2012.09.070 |
| 文献子类 | Article |
| 英文摘要 | A series of 5,6-dihydroxypyrimidine analogs were synthesized and evaluated for their anti-HIV activity in vitro. Among all of the analogs, several compounds exhibited significant anti-HIV activity, especially 1b and 1e, which showed the most potent anti-HIV activity with EC50 values of 0.14 and 0.15 mu M, and TI (therapeutic index) values of >300 and >900, respectively. Further docking studies revealed that the representative compounds 1e and 3a could meet the HIV-1 integrase inhibition minimal requirements of a chelating domain (two metal ions) and an aromatic domain (pi-pi stacking interactions). (C) 2012 Elsevier Ltd. All rights reserved. |
| WOS关键词 | INTEGRASE INHIBITORS ; IN-VITRO ; POTENT ; RALTEGRAVIR ; DISCOVERY ; 4,5-DIHYDROXYPYRIMIDINE ; ACIDS |
| 资助项目 | National Basic Research Program of China[2012CB518005] ; National Natural Science Foundation of China[20721003] ; National Natural Science Foundation of China[81025017] ; National S&T Major Projects[2012ZX09103-101-072] ; Silver Projec[260644] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000310583100025 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277868]  |
| 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 药物发现与设计中心 药理学第一研究室 |
| 通讯作者 | Zheng, Yong-Tang |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai Inst Biol Sci, State Key Lab Drug Res, Shanghai 200031, Peoples R China; 2.Chinese Acad Sci, Kunming Inst Zool, Key Lab Anim Models & Human Dis Mech Chinese Acad, Kunming 650223, Yunnan, Peoples R China; 3.China Pharmaceut Univ, Dept Med Chem, Nanjing, Jiangsu, Peoples R China |
| 推荐引用方式 GB/T 7714 | Guo, Di-Liang,Zhang, Xing-Jie,Wang, Rui-Rui,et al. Structural modifications of 5,6-dihydroxypyrimidines with anti-HIV activity[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2012,22(23):7114-7118. |
| APA | Guo, Di-Liang.,Zhang, Xing-Jie.,Wang, Rui-Rui.,Zhou, Yu.,Li, Zeng.,...&Liu, Hong.(2012).Structural modifications of 5,6-dihydroxypyrimidines with anti-HIV activity.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,22(23),7114-7118. |
| MLA | Guo, Di-Liang,et al."Structural modifications of 5,6-dihydroxypyrimidines with anti-HIV activity".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 22.23(2012):7114-7118. |
入库方式： OAI收割
来源：上海药物研究所
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