Use of Copper(I) Catalyzed Azide Alkyne Cycloaddition (CuAAC) for the preparation of conjugated pyrrolo[2,3-a]carbazole Pim kinase inhibitors - Archive ouverte HAL Accéder directement au contenu
Article Dans Une Revue European Journal of Medicinal Chemistry Année : 2012

Use of Copper(I) Catalyzed Azide Alkyne Cycloaddition (CuAAC) for the preparation of conjugated pyrrolo[2,3-a]carbazole Pim kinase inhibitors

Résumé

We have previously demonstrated that pyrrolo[2,3-a ]carbazole-3-carbaldehydes are potent Pim kinase inhibitors with in vitro antiproliferative activities. In the present study, we report the synthesis of new pyrrolocarbazoles substituted at the N-10 position. When their ability to inhibit Pim kinase activities were evaluated in in vitro assays, we observed that this nitrogen atom can be substituted without loss of Pim-1 and Pim-3 inhibitory potencies. Moreover, when we added afl uorescent dansyl group (compound13), we were able to show that 13penetrates the plasma membrane and enters the cytoplasm.
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Dates et versions

hal-00681025 , version 1 (20-03-2012)

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  • HAL Id : hal-00681025 , version 1

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Boris Letribot, Rufine Akué-Gédu, Niina Santio, Malika El-Ghozzi, Daniel Avignant, et al.. Use of Copper(I) Catalyzed Azide Alkyne Cycloaddition (CuAAC) for the preparation of conjugated pyrrolo[2,3-a]carbazole Pim kinase inhibitors. European Journal of Medicinal Chemistry, 2012, 50, pp.304-310. ⟨hal-00681025⟩
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