Synthesis,Pim kinase inhibitory potencies and in vitro antiproliferative activities of diversely substituted pyrrolo[2,3-a]carbazoles |
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| Authors: | Rufine Akué-Gédu Lionel Nauton Vincent Théry Jenny Bain Philip Cohen Fabrice Anizon Pascale Moreau |
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| Institution: | 1. Clermont Université, Université Blaise Pascal, SEESIB, BP10448, F-63000 Clermont-Ferrand, France;2. CNRS, UMR 6504, SEESIB, F-63177 Aubière, France;3. MRC Protein Phosphorylation Unit, College of Life Sciences, Sir James Black Centre, University of Dundee, Dundee, DD1 5EH Scotland, UK |
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| Abstract: | The synthesis of new pyrrolo2,3-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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