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1-Aryl-tetrahydroisoquinoline analogs as active anti-HIV agents in vitro.

Abstract：

: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 EC(50) values of 8.2, 4.6, and 5.3microM respectively, and the cytotoxicities (CC(50)) of these three compounds were 784.3, 727.3, and 687.3microM, which resulted in SI values larger than 95, 159, and 130 respectively.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Cheng P,Huang N,Jiang ZY,Zhang Q,Zheng YT,Chen JJ,Zhang XM,Ma YB

doi

10.1016/j.bmcl.2008.02.040

subject

Has Abstract

pub_date

2008-04-01 00:00:00

pages

2475-8

issue

7

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(08)00222-9

journal_volume

18

pub_type

杂志文章

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