Synthesis of new pyridazino[4,5-b]indol-4-ones and pyridazin-3(2H)-one analogs as DYRK1A inhibitors

New pyridazino[4,5-b]indol-4-ones and pyridazin-3(2H)-one analogs were synthesized and their inhibitory activities against DYRK1A, CDK5/p25, GSK3α/β and p110-α isoform of PI3K evaluated using harmine as reference. Both furan-2-yl 10 and pyridin-4-yl 19 from the two different series, exhibited submicromolar IC50 against DYRK1A with no activities against the three other kinases. In addition, compound 10 exhibited antiproliferative activities in the Huh-7, Caco2 and MDA-MB-231 cell lines.

Mots clés

4-Oxo-3 4-dihydro-5H-pyridazino[4 5-b]indole Pyridazin-3(2H)-one DYRK1A inhibitors Anti-proliferative effects Synthesis

Domaines

Biochimie [q-bio.BM]

Fichier principal

Synthesis of new pyridazino_accepted.pdf (378.72 Ko)

Origine	Fichiers produits par l'(les) auteur(s)

Muriel Cadieu : Connectez-vous pour contacter le contributeur

https://univ-rennes.hal.science/hal-01086026

Soumis le : vendredi 21 novembre 2014-16:17:27

Dernière modification le : mardi 10 décembre 2024-15:08:32

Archivage à long terme le : lundi 23 février 2015-09:07:46

Dates et versions

hal-01086026 , version 1 (21-11-2014)

Identifiants

HAL Id : hal-01086026 , version 1
DOI : 10.1016/j.bmcl.2014.09.017

Citer

Amélie Bruel, Romain Beneteau, Mylène Chabanne, Olivier Lozach, Rémy Le Guevel, et al.. Synthesis of new pyridazino[4,5-b]indol-4-ones and pyridazin-3(2H)-one analogs as DYRK1A inhibitors. Bioorganic and Medicinal Chemistry Letters, 2014, 24 (21), pp.5037 - 5040. ⟨10.1016/j.bmcl.2014.09.017⟩. ⟨hal-01086026⟩

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