IR@PKUHSC  > 北京大学药学院  > 化学生物学系
学科主题药学
Synthesis and biological evaluation of novel C5 halogen-functionalized S-DABO as potent HIV-1 non-nucleoside reverse transcriptase inhibitors
Qin, Hua1; Liu, Chang2; Guo, Ying3; Wang, Ruiping2; Zhang, Jianfang2; Ma, Liying4; Zhang, Zhili3; Wang, Xiaowei3; Cui, Yuxin1; Liu, Junyi1,3
关键词HIV-1 RT NNRTIs S-DABO analogues Docking
刊名BIOORGANIC & MEDICINAL CHEMISTRY
2010-05-01
DOI10.1016/j.bmc.2010.03.025
18期:9页:3231-3237
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Biochemistry & Molecular Biology ; Chemistry, Medicinal ; Chemistry, Organic
资助者National Science Foundation of China ; Ministry of Science and Technology of China ; National Science Foundation of China ; Ministry of Science and Technology of China
研究领域[WOS]Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry
关键词[WOS]ANTI-HIV-1 ACTIVITY ; RT INHIBITORS ; DERIVATIVES ; DESIGN ; SERIES ; PYRIMIDIN-4(3H)-ONES ; STRAINS ; ANALOGS ; BINDING ; FAMILY
英文摘要

A series of novel S-DABO analogues (4a1-5a12) have been synthesized by an efficient method and evaluated as inhibitors of human immunodeficiency virus type-1 (HIV-1). The biological testing results clearly indicated that the substitution of halogen at the C5 position of pyrimidine ring could increase the anti-HIV-1 RT activity. The most active compounds showed activity in the low micromole range with IC(50) values (IC(50) 0.18-3.03 mu M) comparable to nevirapine (IC(50) 4.12 mu M). The docking showed that a new halogen bond was formed between halogen and carbonyl of TYR188 in the HIV-I RT. (c) 2010 Elsevier Ltd. All rights reserved.

语种英语
所属项目编号20672008 ; 20972011 ; 2005CB523103
资助者National Science Foundation of China ; Ministry of Science and Technology of China ; National Science Foundation of China ; Ministry of Science and Technology of China
WOS记录号WOS:000277083400025
Citation statistics
Cited Times:21[WOS]   [WOS Record]     [Related Records in WOS]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/61855
Collection北京大学药学院_化学生物学系
作者单位1.Peking Univ, State Key Lab Natl & Biomimet Drug, Beijing 100191, Peoples R China
2.Capital Med Univ, Coll Pharmaceut Sci, Beijing 100069, Peoples R China
3.Peking Univ, Sch Pharmaceut Sci, Dept Biol Chem, Beijing 100191, Peoples R China
4.Chinese Ctr Dis Control & Prevent, Natl Ctr AIDS STD Control & Prevent, State Key Lab Infect Dis Prevent & Control, Beijing 100050, Peoples R China
Recommended Citation
GB/T 7714
Qin, Hua,Liu, Chang,Guo, Ying,et al. Synthesis and biological evaluation of novel C5 halogen-functionalized S-DABO as potent HIV-1 non-nucleoside reverse transcriptase inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2010,18(9):3231-3237.
APA Qin, Hua.,Liu, Chang.,Guo, Ying.,Wang, Ruiping.,Zhang, Jianfang.,...&Liu, Junyi.(2010).Synthesis and biological evaluation of novel C5 halogen-functionalized S-DABO as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY,18(9),3231-3237.
MLA Qin, Hua,et al."Synthesis and biological evaluation of novel C5 halogen-functionalized S-DABO as potent HIV-1 non-nucleoside reverse transcriptase inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY 18.9(2010):3231-3237.
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