1-aryl-tetrahydroisoquinoline analogs as active anti-HIV agents in vitro
Cheng, Pi1,3; Huang, Ning2; Jiang, Zhi-Yong1; Zhang, Quan1,3; Zheng, Yong-Tang2; Chen, Ji-Jun1; Zhang, Xue-Mei1; Ma, Yun-Bao1
2008-04-01
发表期刊BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN0960-894X
卷号18期号:7页码:2475-2478
摘要A series of 1-aryl-6,7-dihydroxyl(methoxy)-1,2,3,4-tetrahydroisoquinolines (compounds 1-36) were synthesized via Pictet-Spengler cyclization. All the synthesized compounds were assayed for activities against HIV-1(IIIB) in C8166 cell cultures by MTT method for the first time. The results of the anti-HIV screening revealed that 6,7-dihydroxytetrahydroisoquinolines possessed higher selective index than 6,7-dimethoxyl analogs due to the significantly decreased cytotoxicities. Compounds 6, 24, and 36 showed potent anti-HIV activities with EC50 values of 8.2, 4.6, and 5.3 mu M respectively, and the cytotoxicities (CC50) of these three compounds were 784.3, 727.3, and 687.3 mu M, which resulted in SI values larger than 95, 159, and 130 respectively. (C) 2008 Elsevier Ltd. All rights reserved.
关键词1-aryl-tetrahydroisoquinoline Anti-hiv Activity Pictet-spengler Cyclization
学科领域Chemistry ; Medicinal ; Chemistry ; Organic
DOI10.1016/j.bmcl.2008.02.040
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:000255246300048
引用统计
被引频次:44[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/151853/1901
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 Bot, State Key Lab Phytochem & Plant Resources W China, Kunming 650204, Yunnan, Peoples R China
2.Chinese Acad Sci, Kunming Inst Zoo, Key Lab Anim Models & Human Dis Mech, Lab Mol Immunopharmacol, Kunming 650223, Yunnan, Peoples R China
3.Chinese Acad Sci, Grad Sch, Beijing 100039, Peoples R China
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Cheng, Pi,Huang, Ning,Jiang, Zhi-Yong,et al. 1-aryl-tetrahydroisoquinoline analogs as active anti-HIV agents in vitro[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2008,18(7):2475-2478.
APA Cheng, Pi.,Huang, Ning.,Jiang, Zhi-Yong.,Zhang, Quan.,Zheng, Yong-Tang.,...&Ma, Yun-Bao.(2008).1-aryl-tetrahydroisoquinoline analogs as active anti-HIV agents in vitro.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,18(7),2475-2478.
MLA Cheng, Pi,et al."1-aryl-tetrahydroisoquinoline analogs as active anti-HIV agents in vitro".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 18.7(2008):2475-2478.
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