Synthesis of new dipyrrolo- and furopyrrolopyrazinones related to tripentones and their biological evaluation as potential kinases (CDKs1-5, GSK-3) inhibitors |
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| Authors: | Rochais Christophe Duc Nghia Vu Lescot Elodie Sopkova-de Oliveira Santos Jana Bureau Ronan Meijer Laurent Dallemagne Patrick Rault Sylvain |
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| Affiliation: | Centre d'Etudes et de Recherche sur le Médicament de Normandie, U.F.R. des Sciences Pharmaceutiques, Université de Caen Basse-Normandie, 5 rue Vaubénard, 14032 Caen cedex, France. |
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| Abstract: | We herein describe the synthesis of novel dipyrrolo- and furopyrrolopyrazinones related to highly cytotoxic tripentones and to their oximes. The synthetic pathway involved in particular a Curtius rearrangement and a subsequent cyclisation into the title pyrazinones. The biological evaluation towards various cyclin-dependent kinases (CDKs1-5, GSK-3) highlighted a weak inhibitory activity for the oximes whose SAR was studied by a molecular modeling study. |
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