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题名: 1-aryl-tetrahydroisoquinoline analogs as active anti-HIV agents in vitro
作者: Cheng, Pi1, 3; Huang, Ning2; Jiang, Zhi-Yong1; Zhang, Quan1, 3; Zheng, Yong-Tang2; null(陈纪军)1; Zhang, Xue-Mei1; Ma, Yun-Bao1
刊名: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
关键词: 1-aryl-tetrahydroisoquinoline ; anti-HIV activity ; Pictet-Spengler cyclization
英文摘要: 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.
出版日期: 2008-04-01
卷号: 18, 期号:7, 页码:2475-2478
DOI标识: 10.1016/j.bmcl.2008.02.040
语种: 英语
ISSN号: 0960-894X
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内容类型: 期刊论文
URI标识: http://ir.kib.ac.cn/handle/151853/1901
Appears in Collections:植物化学与西部植物资源持续利用国家重点实验室_期刊论文

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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

Recommended Citation:
Cheng, P; Huang, N; Jiang, ZY; Zhang, Q; Zheng, YT; Chen, JJ; Zhang, XM; Ma, YB.1-aryl-tetrahydroisoquinoline analogs as active anti-HIV agents in vitro,BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2008,18(7):2475-2478
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