中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
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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