A1 Refereed original research article in a scientific journal

Use of copper(I) catalyzed azide alkyne cycloaddition (CuAAC) for the preparation of conjugated pyrrolo[2,3-a]carbazole Pim kinase inhibitors

Authors: Letribot Boris, Akué-Gédu Rufine, Santio Niina M, El-Ghozzi Malika, Avignant Daniel, Cisnetti Federico, Koskinen Päivi J, Gautier Arnaud, Anizon Fabrice, Moreau Pascale

Publisher: ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER

Publication year: 2012

Journal: European Journal of Medicinal Chemistry

Journal acronym: Eur J Med Chem.

Volume: 50

First page : 304

Last page: 310

Number of pages: 7

ISSN: 0223-5234

DOI: https://doi.org/10.1016/j.ejmech.2012.02.009

Web address : http://dx.doi.org/10.1016/j.ejmech.2012.02.009

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 a fluorescent dansyl group (compound 13), we were able to show that 13 penetrates the plasma membrane and enters the cytoplasm.