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. 2004 Mar 22;14(6):1543-6.
doi: 10.1016/j.bmcl.2003.12.095.

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

Mickaël Montembault  1 , Giang Vo-Thanh, Abdallah Deyine, Valérie Fargeas, Monique Villiéras, Ané Adjou, Didier Dubreuil, Didier Esquieu, Catherine Grégoire, Sandrine Opi, Jean-Marie Péloponèse, Grant Campbell, Jennifer Watkins, Jean de Mareuil, Anne-Marie Aubertin, Christian Bailly, Erwann Loret, Jacques Lebreton
Affiliations

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

Mickaël Montembault et al. Bioorg Med Chem Lett. .

Abstract

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.

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