Structural modifications of 5,6-dihydroxypyrimidines with anti-HIV activity
文献类型：期刊论文
| 作者 | Guo DL1,2; Zhang XJ3; Wang RR3; Zhou Y1; Li Z1; Xu JY2; Chen KX1,2; Zheng YT[*]3; Liu H[*]1,2 |
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2012 |
| 卷号 | 22期号:23页码:7114-7118 |
| 关键词 | Dihydroxypyrimidine Synthesis HIV Integrase inhibitor Docking study |
| 通讯作者 | zhengyt@mail.kiz.ac.cn ; hliu@mail.shcnc.ac.cn |
| 合作状况 | 其它 |
| 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). |
| 收录类别 | SCI |
| 资助信息 | We gratefully acknowledge financial support from National Ba- sic Research Program of China (Grants 2012CB518005 and 2012CB518005), the National Natural Science Foundation of China (Grants 20721003 and 81025017), National S&T Major Projects (2012ZX09103-101-072) and Silver Project (260644). |
| 语种 | 英语 |
| WOS记录号 | WOS:000310583100025 |
| 公开日期 | 2013-04-09 |
| 源URL | [http://159.226.149.42:8088/handle/152453/7319]  |
| 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 Drug Research, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai, PR China 2.Department of Medicinal Chemistry, China Pharmaceutical University, 24 TongjiaXiang, Nanjing, PR China 3.Key Laboratory of Animal Models and Human Disease Mechanisms of Chinese Academy of Sciences and Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, Yunnan, China |
| 推荐引用方式 GB/T 7714 | Guo DL,Zhang XJ,Wang RR,et al. Structural modifications of 5,6-dihydroxypyrimidines with anti-HIV activity[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2012,22(23):7114-7118. |
| APA | Guo DL.,Zhang XJ.,Wang RR.,Zhou Y.,Li Z.,...&Liu H[*].(2012).Structural modifications of 5,6-dihydroxypyrimidines with anti-HIV activity.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,22(23),7114-7118. |
| MLA | Guo DL,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：昆明动物研究所
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