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Synthesis and Biological Evaluation of Novel 2-Arylalkylthio-5-iodine-6-substituted-benzyl-pyrimidine-4(3H)-ones as Potent HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors
Zhang, Liang1; Tang, Xiaowan1; Cao, Yuanyuan1; Wu, Shaotong1; Zhang, Yu1; Zhao, Jianxiong1; Guo, Ying1; Tian, Chao1; Zhang, Zhili1; Liu, Junyi1,2; Wang, Xiaowei1
关键词HIV NNRTIs S-DABOs IC50 docking
刊名MOLECULES
2014-06-01
DOI10.3390/molecules19067104
19期:6页:7104-7121
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Organic
研究领域[WOS]Chemistry
关键词[WOS]IMMUNODEFICIENCY-VIRUS TYPE-1 ; S-DABO DERIVATIVES ; ANTI-HIV-1 ACTIVITY ; URACIL DERIVATIVES ; IN-VITRO ; DESIGN ; RESISTANCE ; DRUGS
英文摘要

A novel series of 2-arylalkylthio-5-iodine-6-substitutedbenzyl-pyrimidine-4(3H)-ones (S-DABOs) 8a-x had been synthesized via an efficient method. Their biological activity against HIV virus and RT assay were evaluated. Some compounds, especially 8h, 8l and 8n, displayed promising activity against HIV-1 RT with IC50 values in a range of 0.41 mu M to 0.71 mu M, which were much better than that of nevirapine. Molecular modeling studies revealed that the binding mode would be affected via forming an additional hydrogen bond by incorporating an oxygen atom on the C-2 side chain. The biological activity was in accordance with the docking results.

语种英语
WOS记录号WOS:000338586700012
项目编号20972011 ; 21042009 ; 21172014 ; 2009ZX09301-010
资助机构Foundation of China ; Ministry of Science and Technology of China
引用统计
被引频次:9[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/62935
专题北京大学药学院_化学生物学系
北京大学药学院
北京大学第三临床医学院_麻醉科
作者单位1.Peking Univ, Dept Biol Chem, Sch Pharmaceut Sci, Beijing 100191, Peoples R China
2.Peking Univ, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
推荐引用方式
GB/T 7714
Zhang, Liang,Tang, Xiaowan,Cao, Yuanyuan,et al. Synthesis and Biological Evaluation of Novel 2-Arylalkylthio-5-iodine-6-substituted-benzyl-pyrimidine-4(3H)-ones as Potent HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors[J]. MOLECULES,2014,19(6):7104-7121.
APA Zhang, Liang.,Tang, Xiaowan.,Cao, Yuanyuan.,Wu, Shaotong.,Zhang, Yu.,...&Wang, Xiaowei.(2014).Synthesis and Biological Evaluation of Novel 2-Arylalkylthio-5-iodine-6-substituted-benzyl-pyrimidine-4(3H)-ones as Potent HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors.MOLECULES,19(6),7104-7121.
MLA Zhang, Liang,et al."Synthesis and Biological Evaluation of Novel 2-Arylalkylthio-5-iodine-6-substituted-benzyl-pyrimidine-4(3H)-ones as Potent HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors".MOLECULES 19.6(2014):7104-7121.
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