Synthesis and biological evaluation of naphthyl phenyl ethers (NPEs) as novel nonnucleoside HIV-1 reverse transcriptase inhibitors
文献类型:期刊论文
作者 | Gu SX1; Zhang X3; Zheng YT3; Yang SQ1; Chen FE[*]1,2; He QQ1; Yang LM3; Ma XD1 |
刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS |
出版日期 | 2011 |
卷号 | 19期号:14页码:4220-4226 |
关键词 | HIV-1 reverse transcriptase NNRTIs NPEs SAR Anti-HIV activity |
通讯作者 | rfchen@fudan.edu.cn |
合作状况 | 其它 |
英文摘要 | A novel series of naphthyl phenyl ether analogues (NPEs) have been synthesized and evaluated for their in vitro activities against HIV in C8166 cells. Most of the compounds exhibited moderate to excellent anti-HIV activities. Among them the most active compound 12o showed excellent activities against wild-type HIV-1 with an EC(50) value of 4.60 nM, along with moderate activities against the double mutant strain HIV-1(IIIB) A17 (K103N+Y181C) and HIV-2 strain ROD with an EC(50) value of 0.82 and 4.40 mu M, respectively. Preliminary structure-activity relationship (SAR) among the newly synthesized NPEs was also investigated. |
资助信息 | This work was supported by grants from the National Natural Science Foundation of China (No. 30672536), the Knowledge Inno- vation Program of CAS (KSCX2-YW-R-185), 973 program (2009CB522306) and Eleventh Five-Year Key Scientific and Tech- nological Program of China (2009ZX09501-029). |
收录类别 | SCI |
语种 | 英语 |
源URL | [http://159.226.149.26:8080/handle/152453/10417] |
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.Department of Chemistry, Fudan University, Shanghai 200433, People’s Republic of China 2.Institute of Biomedical Science, Fudan University, Shanghai 200433, People’s Republic of China 3.Key Laboratory of Animal Models and Human Disease Mechanisms of Chinese Academy of Sciences & Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, People’s Republic of China |
推荐引用方式 GB/T 7714 | Gu SX,Zhang X,Zheng YT,et al. Synthesis and biological evaluation of naphthyl phenyl ethers (NPEs) as novel nonnucleoside HIV-1 reverse transcriptase inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2011,19(14):4220-4226. |
APA | Gu SX.,Zhang X.,Zheng YT.,Yang SQ.,Chen FE[*].,...&Ma XD.(2011).Synthesis and biological evaluation of naphthyl phenyl ethers (NPEs) as novel nonnucleoside HIV-1 reverse transcriptase inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,19(14),4220-4226. |
MLA | Gu SX,et al."Synthesis and biological evaluation of naphthyl phenyl ethers (NPEs) as novel nonnucleoside HIV-1 reverse transcriptase inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 19.14(2011):4220-4226. |
入库方式: OAI收割
来源:昆明动物研究所
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