Identification of pyrrolo[2,3-g]indazoles as new Pim kinase inhibitors. - Archive ouverte HAL Accéder directement au contenu
Article Dans Une Revue Bioorganic and Medicinal Chemistry Letters Année : 2013

Identification of pyrrolo[2,3-g]indazoles as new Pim kinase inhibitors.

Résumé

The synthesis and Pim kinase inhibition potency of a new series of pyrrolo[2,3-g]indazole derivatives is described. The results obtained in this preliminary structure–activity relationship study pointed out that sub-micromolar Pim-1 and Pim-3 inhibitory potencies could be obtained in this series, more particularly for compounds 10 and 20, showing that pyrrolo[2,3-g]indazole scaffold could be used for the development of new potent Pim kinase inhibitors. Molecular modeling experiments were also performed to study the binding mode of these compounds in Pim-3 ATP-binding pocket.

Domaines

Chimie organique

Dates et versions

hal-01089114 , version 1 (01-12-2014)

Identifiants

Citer

Laurent Gavara, Virginie Suchaud, Lionel Nauton, Vincent Théry, Fabrice Anizon, et al.. Identification of pyrrolo[2,3-g]indazoles as new Pim kinase inhibitors.. Bioorganic and Medicinal Chemistry Letters, 2013, 23 (8), pp.2298-2301. ⟨10.1016/j.bmcl.2013.02.074⟩. ⟨hal-01089114⟩
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