Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1355922 | Bioorganic Chemistry | 2014 | 8 Pages |
•New pyrrolo[2,3-a]carbazoles were synthesized.•Inhibitory potencies were determined toward Pim kinases (Pim-1, Pim-2 and Pim-3).•High inhibitory potencies were found toward Pim-1 and Pim-3.•Two potent Pim inhibitors exhibited apoptosis–inducing activity toward IPC-81 cells.
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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