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
Source PublicationBIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN0960-894X
Volume18Issue:7Pages:2475-2478
AbstractA 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.
Keyword1-aryl-tetrahydroisoquinoline Anti-hiv Activity Pictet-spengler Cyclization
Subject AreaChemistry ; Medicinal ; Chemistry ; Organic
DOI10.1016/j.bmcl.2008.02.040
Indexed BySCI
Language英语
WOS Research AreaPharmacology & Pharmacy ; Chemistry
WOS SubjectChemistry, Medicinal ; Chemistry, Organic
WOS IDWOS:000255246300048
Citation statistics
Cited Times:45[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://ir.kib.ac.cn/handle/151853/1901
Collection植物化学与西部植物资源持续利用国家重点实验室
Affiliation1.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
Recommended Citation
GB/T 7714
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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