Synthesis and biological evaluation of N-acetyl-beta-aryl-1,2-didehydroethylamines as new HIV-1 RT inhibitors in vitro
Cheng, Pi; Jiang, Zhi-Yong; Wang, Rul-Rul; Zhang, Xue-Mel; Wang, Qian; Zheng, Yong-Tang; Zhou, Jun; Chen, Ji-Jun
2007-08-15
发表期刊BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN0960-894X
卷号17期号:16页码:4476-4480
摘要A variety of N-acetyl-o-aryl-1,2-didehydroethylamines were synthesized by direct reduction-acetylation of beta-aryl-nitroolefins and assayed as HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) for the first time. Compound 7a exhibited a TI value of > 13.2 with CC50 value of > 0.787 mM in C8166 cells. This structure-activity relationship (SAR) study provided a new lead for design and discovery of more potent and selective analogues act as NNRTIs. (c) 2007 Elsevier Ltd. All rights reserved.
关键词Beta-aryl-nitroolefin N-acetyl-beta-aryl-1 Nnrtis 2-didehydroethylamine Anti-hiv-1 Rt Activity
学科领域Chemistry ; Medicinal ; Chemistry ; Organic
DOI10.1016/j.bmcl.2007.06.008
收录类别SCI
语种英语
WOS研究方向Pharmacology & Pharmacy ; Chemistry
WOS类目Chemistry, Medicinal ; Chemistry, Organic
WOS记录号WOS:000248877800014
引用统计
被引频次:20[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.kib.ac.cn/handle/151853/2045
专题植物化学与西部植物资源持续利用国家重点实验室
作者单位1.Chinese Acad Sci, Kunming Inst Zool, Key Lab Anim Models & Human Dis Mech, Lab Mol Immunopharmacol, Kunming 650223, Peoples R China
2.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resource W China, Kunming 650204, Peoples R China
3.Chinese Acad Sci, Joint Lab Antiviral Nat Med, Kunming 650204, Peoples R China
4.Chinese Acad Sci, Grad Sch, Beijing 100039, Peoples R China
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Cheng, Pi,Jiang, Zhi-Yong,Wang, Rul-Rul,et al. Synthesis and biological evaluation of N-acetyl-beta-aryl-1,2-didehydroethylamines as new HIV-1 RT inhibitors in vitro[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2007,17(16):4476-4480.
APA Cheng, Pi.,Jiang, Zhi-Yong.,Wang, Rul-Rul.,Zhang, Xue-Mel.,Wang, Qian.,...&Chen, Ji-Jun.(2007).Synthesis and biological evaluation of N-acetyl-beta-aryl-1,2-didehydroethylamines as new HIV-1 RT inhibitors in vitro.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,17(16),4476-4480.
MLA Cheng, Pi,et al."Synthesis and biological evaluation of N-acetyl-beta-aryl-1,2-didehydroethylamines as new HIV-1 RT inhibitors in vitro".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 17.16(2007):4476-4480.
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