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• W3023404927 endingPage "89" @default.
• W3023404927 startingPage "89" @default.
• W3023404927 abstract "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." @default.
• W3023404927 created "2020-05-13" @default.
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• W3023404927 date "2020-05-09" @default.
• W3023404927 modified "2023-10-17" @default.
• W3023404927 title "Exploring Kinase Inhibition Properties of 9H-pyrimido[5,4-b]- and [4,5-b]indol-4-amine Derivatives" @default.
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• W3023404927 doi "https://doi.org/10.3390/ph13050089" @default.
• W3023404927 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/7281298" @default.
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