1-aryl-tetrahydroisoquinoline analogs as active anti-HIV agents in vitro

doi:10.1016/j.bmcl.2008.02.040

	1-aryl-tetrahydroisoquinoline analogs as active anti-HIV agents in vitro
	Cheng, Pi 1,3; Huang, Ning 2; Jiang, Zhi-Yong 1; Zhang, Quan 1,3; Zheng, Yong-Tang 2; Chen, Ji-Jun1 ; Zhang, Xue-Mei1 ; Ma, Yun-Bao 1
	2008-04-01
发表期刊	BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN	0960-894X
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
DOI	10.1016/j.bmcl.2008.02.040
收录类别	SCI
语种	英语
WOS记录号	WOS:000255246300048
引用统计
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
推荐引用方式 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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