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Article Dans Une Revue Journal of Medicinal Chemistry Année : 2009

Novel Organic Proteasome Inhibitors Identified by Virtual and in Vitro Screening

Résumé

Proteasome inhibition is a promising strategy for treating cancers. Herein, we report the discovery of novel drug-like inhibitors of mammalian proteasome 20S using a multistep structure-based virtual ligand screening strategy. Sulfone- or piperazine-containing hits essentially belong to the under-represented class of noncovalent and nonpeptidic proteasome inhibitors. Several of our compounds act in the micromolar range and are cytotoxic on human tumoral cell lines. Optimization of these molecules could lead to better anticancer therapy.

Domaines

Chimie organique
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Dates et versions

hal-00842659 , version 1 (09-07-2013)

Identifiants

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Basse Nicolas, Matthieu Montes, Xavier Maréchal, Lixian Qin, Michelle Bouvier-Durand, et al.. Novel Organic Proteasome Inhibitors Identified by Virtual and in Vitro Screening. Journal of Medicinal Chemistry, 2009, 53 (1), pp.509-513. ⟨10.1021/jm9011092⟩. ⟨hal-00842659⟩
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