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Synthesis and Biological Evaluation of Thienopyrrolizines, a New Family of CDK/GSK-3 Inhibitors
Article de revue   Avec comité de lecture

Synthesis and Biological Evaluation of Thienopyrrolizines, a New Family of CDK/GSK-3 Inhibitors

Christophe Rochais, Elodie Lescot, Vincent Lisowski, Alban Lepailleur, Jana sopkova-de oliveira Santos, Ronan Bureau, Patrick Dallemagne, Laurent Meijer et Sylvain Rault
Journal of enzyme inhibition and medicinal chemistry, Vol.19(6), pp.585-593
12/2004
DOI: https://doi.org/10.1080/14756360400004565
PMID: 15662962

Résumé

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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