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Synthesis and biological evaluation of novel 2-arylalkylthio-4-amino-6-benzyl pyrimidines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors
Qin, Hua2; Liu, Chang2; Zhang, Jianfang2; Guo, Ying1; Zhang, Siwei3; Zhang, Zhili1; Wang, Xiaowei1; Zhang, Liangren3; Liu, Junyi1,3
关键词Non-nucleoside reverse transcriptase inhibitors (NNRTIs) 2-Aryalkylthio-4-amino-6-benzylpyrimidines Docking
刊名BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
2010-05-01
DOI10.1016/j.bmcl.2009.04.051
20期:9页:3003-3005
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Medicinal ; Chemistry, Organic
资助者National Sciences Foundation of China ; Ministry of Education of China ; National Sciences Foundation of China ; Ministry of Education of China
研究领域[WOS]Pharmacology & Pharmacy ; Chemistry
关键词[WOS]STRUCTURE-BASED DESIGN ; ANTI-HIV-1 ACTIVITY ; POSITIONAL ADAPTABILITY ; CONFORMATIONAL-CHANGES ; DERIVATIVES ; SERIES ; BINDING
英文摘要

Novel 2-aryalkylthio-4-amino-6-benzylpyrimidines (3a-i), which can be considered as S-DABO and TMC-125 analogue hybrid molecules, have been designed and synthesized as inhibitors of HIV-1 RT. The results clearly indicated that the changes at the N(3)/C(4) position of pyrimidine ring could affect the hydrogen bonds strength and number between N(3)/C(4) and the Lys101 residue which are indispensable for anti-HIV-1 RT activity. The biological activity results are also in accordance with the docking study. (C) 2009 Elsevier Ltd. All rights reserved.

语种英语
所属项目编号20672008
资助者National Sciences Foundation of China ; Ministry of Education of China ; National Sciences Foundation of China ; Ministry of Education of China
WOS记录号WOS:000276816600068
引用统计
被引频次:13[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/400002259/62905
专题北京大学药学院_化学生物学系
作者单位1.Peking Univ, Sch Pharmaceut Sci, Dept Biol Chem, Beijing 100191, Peoples R China
2.Capital Med Univ, Coll Pharmaceut Sci, Beijing 100069, Peoples R China
3.Peking Univ, State key Lab Natl & Biomimet Drug, Beijing 100191, Peoples R China
推荐引用方式
GB/T 7714
Qin, Hua,Liu, Chang,Zhang, Jianfang,et al. Synthesis and biological evaluation of novel 2-arylalkylthio-4-amino-6-benzyl pyrimidines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2010,20(9):3003-3005.
APA Qin, Hua.,Liu, Chang.,Zhang, Jianfang.,Guo, Ying.,Zhang, Siwei.,...&Liu, Junyi.(2010).Synthesis and biological evaluation of novel 2-arylalkylthio-4-amino-6-benzyl pyrimidines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,20(9),3003-3005.
MLA Qin, Hua,et al."Synthesis and biological evaluation of novel 2-arylalkylthio-4-amino-6-benzyl pyrimidines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 20.9(2010):3003-3005.
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