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
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
Indexed BySCI
WOS Research AreaPharmacology & Pharmacy ; Chemistry
WOS SubjectChemistry, Medicinal ; Chemistry, Organic
WOS IDWOS:000255246300048
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Cited Times:45[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
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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