2. Academic Validation
  3. Synthesis, Pim kinase inhibitory potencies and in vitro antiproliferative activities of diversely substituted pyrrolo[2,3-a]carbazoles

Synthesis, Pim kinase inhibitory potencies and in vitro antiproliferative activities of diversely substituted pyrrolo[2,3-a]carbazoles

  • Bioorg Med Chem. 2010 Sep 15;18(18):6865-73. doi: 10.1016/j.bmc.2010.07.036.
Rufine Akué-Gédu 1,  Lionel Nauton,  Vincent Théry,  Jenny Bain,  Philip Cohen,  Fabrice Anizon,  Pascale Moreau
Affiliations

Affiliation

  • 1 Clermont Université, Université Blaise Pascal, SEESIB, BP10448, F-63000 Clermont-Ferrand, France.
PMID: 20728368 DOI: 10.1016/j.bmc.2010.07.036
Abstract

The synthesis of new pyrrolo[2,3-a]carbazole derivatives diversely substituted at the C-6 to C-9 positions is described. These compounds were tested for their kinase inhibitory potencies toward three kinases (Pim-1, Pim-2, Pim-3) as well as for their in vitro antiproliferative activities toward a human fibroblast primary culture and three human solid Cancer cell lines (PC3, DU145, and PA 1). Moreover, molecular docking studies were performed to explain the enhanced inhibitory activity of the most active compound 3d.

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