Synthesis of dipyrrolo[3,4-a:3,4-c]carbazoles: new kinase inhibitors |
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| Authors: | Elisabeth Pereira Ali Youssef Malika El-Ghozzi Daniel Avignant Jennifer Bain Michelle Prudhomme Fabrice Anizon Pascale Moreau |
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| Institution: | 1. Clermont Université, Université Blaise Pascal, Institut de Chimie de Clermont-Ferrand, BP 10448, 63000 Clermont-Ferrand, France;2. CNRS, UMR 6296, ICCF, BP 80026, 63171 Aubière, France;3. MRC Protein Phosphorylation and Ubiquitylation Unit, College of Life Sciences, Sir James Black Centre, University of Dundee, Dundee, DD1 5EH Scotland, UK |
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| Abstract: | Two dipyrrolo3,4-a:3,4-c]carbazole stereoisomers were unexpectedly obtained by Diels–Alder dimerization of 3-indolylmaleimide. Three dimensional structures of both stereoisomers were confirmed by X-ray analysis. Moreover compound 4 inhibits protein kinases in vitro, especially Pim-3, in the sub-micromolar range. |
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| Keywords: | Dipyrrolo[3 4-a:3 4-c]carbazole Diels&ndash Alder reaction Cycloaddition In vitro kinase inhibition |
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