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Correction: McLoughlin, E.C.; O’Boyle, N.M. Colchicine-Binding Site Inhibitors from Chemistry to Clinic: A Review. Pharmaceuticals 2020, 13, 8
Open AccessCommunication

Exploring Kinase Inhibition Properties of 9H-pyrimido[5,4-b]- and [4,5-b]indol-4-amine Derivatives

Normandie Université, UNIROUEN, INSA Rouen, CNRS, COBRA UMR 6014, F-76000 Rouen, France
Université de Nantes, Cibles et Médicaments des Infections et du Cancer, IICiMed, EA 1155, F-44000 Nantes, France
Station Biologique de Roscoff, Protein Phosphorylation & Human Disease Group, 29680 Roscoff, France
Perha Pharmaceuticals, Perharidy Peninsula, 29680 Roscoff, France
Authors to whom correspondence should be addressed.
Pharmaceuticals 2020, 13(5), 89;
Received: 10 April 2020 / Revised: 1 May 2020 / Accepted: 8 May 2020 / Published: 9 May 2020
We previously highlighted the interest in 6,5,6-fused tricyclic analogues of 4-aminoquinazolines as kinase inhibitors in the micromolar to the nanomolar range of IC50 values. For the generation of chemical libraries, the formamide-mediated cyclization of the cyanoamidine precursors was carried out under microwave irradiation in an eco-friendly approach. In order to explore more in-depth the pharmacological interest in such tricyclic skeletons, the central five member ring, i.e., thiophène or furan, was replaced by a pyrrole to afford 9H-pyrimido[5,4-b]- and [4,5-b]indol-4-amine derivatives inspired from harmine. The inhibitory potency of the final products was determined against four protein kinases (CDK5/p25, CK1δ/ε, GSK3α/β, and DYRK1A). As a result, we have identified promising compounds targeting CK1δ/ε and DYRK1A and displaying micromolar and submicromolar IC50 values. View Full-Text
Keywords: microwave-assisted chemistry; protein kinases; CK1; DYRK1A; CDK5; GSK-3 microwave-assisted chemistry; protein kinases; CK1; DYRK1A; CDK5; GSK-3
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Loidreau, Y.; Dubouilh-Benard, C.; Nourrisson, M.-R.; Loaëc, N.; Meijer, L.; Besson, T.; Marchand, P. Exploring Kinase Inhibition Properties of 9H-pyrimido[5,4-b]- and [4,5-b]indol-4-amine Derivatives. Pharmaceuticals 2020, 13, 89.

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