Novel 9-oxo-thiazolo[5,4-f]quinazoline-2-carbonitrile derivatives as dual cyclin-dependent kinase 1 (CDK1)/glycogen synthase kinase-3 (GSK-3) inhibitors: synthesis, biological evaluation and molecular modeling studies |
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| Authors: | Logé Cédric Testard Alexandra Thiéry Valérie Lozach Olivier Blairvacq Mélina Robert Jean-Michel Meijer Laurent Besson Thierry |
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| Affiliation: | Université de Nantes, Nantes Atlantique Universités, Biomolécules et Cibles Thérapeutiques, Département de Pharmacochimie, BioCiT, UPRES EA 1155, UFR Sciences Pharmaceutiques, Nantes Cedex 1, France. cedric.loge@univ-nantes.fr |
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| Abstract: | Continuous efforts in microwave-assisted synthesis and the structure-activity relationships' (SARs) studies of novel modified 9-oxo-thiazolo[5,4-f]quinazoline-2-carbonitriles, allowed identification of new amidine and imidate derivatives as potent and dual CDK1/GSK-3 inhibitors. Combination of lead optimization and molecular modeling studies allowed identification of a dual CDK1/GSK-3 inhibitor (compound 13d) with submicromolar values. |
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| Keywords: | CDK1 inhibitor GSK-3 inhibitor Molecular modeling Microwave-assisted chemistry Quinazolinones |
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