New N-1,N-10 bridged pyrrolo[2,3-a]carbazole-3-carbaldehyde: synthesis and biological activities. - Archive ouverte HAL Accéder directement au contenu
Article Dans Une Revue Bioorganic Chemistry Année : 2014

New N-1,N-10 bridged pyrrolo[2,3-a]carbazole-3-carbaldehyde: synthesis and biological activities.

Résumé

The synthesis of new pyrrolocarbazoles substituted at N-1/N-10 positions is described. All the compounds tested demonstrated moderate to high Pim-1/Pim-3 kinase inhibitory potency. The most active inhibitors identified in this series (3, 17) have an alkyl chain bridging the N-1 and N-10 positions. These compounds (3, 17) exhibited apoptosis–inducing activity toward acute myeloid leukemia IPC-81 cells, but not toward normal fibroblasts.
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Dates et versions

hal-01077457 , version 1 (24-10-2014)

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Francis Giraud, Marion Bourhis, Lionel Nauton, Vincent Théry, Lars Herfindal, et al.. New N-1,N-10 bridged pyrrolo[2,3-a]carbazole-3-carbaldehyde: synthesis and biological activities.. Bioorganic Chemistry, 2014, 57, pp.108-115. ⟨10.1016/j.bioorg.2014.09.004⟩. ⟨hal-01077457⟩
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