Journal
MOLECULES
Volume 21, Issue 5, Pages -Publisher
MDPI AG
DOI: 10.3390/molecules21050578
Keywords
thiazolo[5,4-f]quinazolin-9(8H)-ones; multi-target-directed ligand; protein kinases; microwave-assisted synthesis; CDK5; GSK-3; CLK1; CK1; DYRK1A
Funding
- MESR (French Ministere de l'Enseignement Superieur & de la Recherche)
- LABEX SynOrg [ANR-11-LABX-0029]
- 'Fonds Unique Interministeriel (FUI) TRIAD (LM) projects
- Fondation Jerome Lejeune
- FP7-KBBE grant (BlueGenics)
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A library of thirty novel thiazolo[5,4-f]quinazolin-9(8H)-one derivatives belonging to four series designated as 12, 13, 14 and 15 was efficiently prepared, helped by microwave-assisted technology when required. The efficient multistep synthesis of methyl 6-amino-2-cyano-benzo[d]thiazole-7-carboxylate (1) has been reinvestigated and performed on a multigram scale. The inhibitory potency of the final products against five kinases involved in Alzheimer's disease was evaluated. This study demonstrates that some molecules of the 12 and 13 series described in this paper are particularly promising for the development of new multi-target inhibitors of kinases.
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