A possible improvement for structure-based drug design illustrated by the discovery of a Tat HIV-1 inhibitor

被引：12

作者：

Montembault, M

Vo-Thanh, G

Deyine, A

Fargeas, V

Villiéras, M

Adjou, A

Dubreuil, D

Esquieu, D

Grégoire, C

Opi, S

Péloponèse, JM

Campbell, G

Watkins, J

de Mareuil, J

Aubertin, AM

Bailly, C

Loret, E

Lebreton, J

机构：

[1] Fac Sci, CNRS, UMR 6513, Organ Synth Lab, F-44322 Nantes 3, France

[2] Fac Tech Sci, Chim Organ Struct Lab, Abidjan, Cote Ivoire

[3] Univ Med, CNRS, FRE, Fac Pharm, F-13385 Marseille 5, France

[4] Inst Virol, INSERM, U 74, F-67000 Strasbourg, France

[5] INSERM, U 524, F-59045 Lille, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 06期

关键词：

HIV; inhibitor; Tat protein;

D O I：

10.1016/j.bmcl.2003.12.095

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The HIV-1 Tat protein is a promising target for AIDS therapy, due to its extra-cellular roles against the immune system. From the 2D-NMR structure of Tat, we have designed molecules, called TDS, able to bind to Tat and inhibit HIV-1 replication in vitro. This new family of antivirals is composed of a triphenylene aromatic ring substituted with at least one carbon chain bearing a succinimide group. These ligands are prepared from triphenylene or 2,6, 10-trimethylphenylene in 3-6 steps depending on the target molecule. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：1543 / 1546

页数：4

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