Synthesis and Biological Evaluation of Thienopyrrolizines,a New Family of CDK/GSK-3 Inhibitors |
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| Authors: | Christophe Rochais Elodie Lescot Vincent Lisowski Alban Lepailleur Jana sopkova-de oliveira Santos Ronan Bureau |
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| Affiliation: | Centre d'Etudes et de Recherche sur le Médicament de Normandie, Université de Caen Basse Normandie, 5 rue Vaubénard, 14032, Caen cedex, France |
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| Abstract: | Fifteen new thieno[2,3-b]- and thieno[3,4-b]pyrrolizines were synthesized and tested against two protein kinases, CDK1/cyclin B and GSK-3. Among these compounds, 3-(3-hydroxy-4-methoxyphenyl)-8H-thieno[2,3-b]pyrrolizin-8-one 4g was identified as a moderate inhibitor of these kinases. Its molecular modeling study brought to the fore the pivotal role of the 2-methoxyphenol grouping and the interest in replacing it by bioisosteric moieties in future pharmacomodulations. |
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| Keywords: | Thieno[2,3-b]pyrrolizines Thieno[3,4-b]pyrrolizines Protein kinases CDK1/cyclin B GSK-3 Phosphorylation |
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