Synthesis and biological evaluation of novel coumarin-based inhibitors of Cdc25 phosphatases |
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Authors: | Sergio Valente Emilie Bana Elodie Viry Denyse Bagrel Gilbert Kirsch |
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Institution: | Laboratoire d’Ingénierie Moléculaire et Biochimie Pharmacologique, Institut Jean Barriol, Université Paul Verlaine, FR CNRS 2843, 1 Boulevard Arago, 57070 Metz, France |
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Abstract: | The cell division cycle 25 (Cdc25) family of proteins are dual specificity phosphatases that activate cyclin-dependent kinase (CDK) complexes, which in turn regulate progression through the cell division cycle. Overexpression of Cdc25 proteins has been reported in a wide variety of cancers; their inhibition may thus represent a novel approach for the development of anticancer therapeutics. Herein we report new coumarin-based scaffolds endowed with a selective inhibition against Cdc25A and Cdc25C, being 6a and 6d the most efficient inhibitors and worthy of further investigation as anticancer agents. |
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