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Article Dans Une Revue Bioorganic and Medicinal Chemistry Letters Année : 2004

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

Résumé

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.

Dates et versions

hal-02137964 , version 1 (23-05-2019)

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Mickaël Montembault, Giang Vo-Thanh, Abdallah Deyine, Valérie Fargeas, Monique Villiéras, et al.. A possible improvement for structure-based drug design illustrated by the discovery of a Tat HIV-1 inhibitor. Bioorganic and Medicinal Chemistry Letters, 2004, 14 (6), pp.1543-1546. ⟨10.1016/j.bmcl.2003.12.095⟩. ⟨hal-02137964⟩
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