Synthesis and biological activities of aminopyrimidyl-indoles structurally related to meridianins |
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| Authors: | Rufine Akue-Gedu Eric Debiton Yoan Ferandin Laurent Meijer Michelle Prudhomme Fabrice Anizon Pascale Moreau |
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| Institution: | 1. Clermont Université, Université Blaise Pascal, SEESIB, 24 avenue des Landais, F-63177 Aubière, France;2. CNRS, UMR 6504, F-63177 Aubière, France;3. Clermont Université, Université d’Auvergne, Centre Jean Perrin, EA 4231, F-63005 Clermont-Ferrand, France;4. CNRS, Protein Phosphorylation & Human Disease Group, Station Biologique, BP 74, 29682 Roscoff, France |
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| Abstract: | The synthesis of new meridianin derivatives substituted at the C-5 position of the 2-aminopyrimidine ring by various aryl groups and substituted or not by a methyl group on the indole nitrogen is described. These compounds were tested for their kinase inhibitory potencies toward five kinases (CDK5/p25, CK1δ/ε, GSK-3α/β, Dyrk1A and Erk2) as well as their in vitro antiproliferative activities toward a human fibroblast primary culture and two human solid cancer cell lines (MCF-7 and PA 1). |
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