Journal
MOLECULES
Volume 23, Issue 9, Pages -Publisher
MDPI
DOI: 10.3390/molecules23092181
Keywords
thiazolo[5,4-f]quinazolin-9(8H)-ones; microwave-assisted synthesis; C-H arylation; protein kinases; DYRK1A; CDK5; GSK-3; CLK1; CK1
Funding
- MESR (French Ministere de l'Enseignement Superieur & de la Recherche)
- LABEX SynOrg [ANR-11-LABX-0029]
- Fonds Unique Interministeriel (FUI) TRIAD project
- Conseil Regional de Bretagne
- Fondation Jerome Lejeune
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Efficient metal catalyzed C-H arylation of 8-alkyl-thiazolo[5,4-f]-quinazolin-9-ones was explored for SAR studies. Application of this powerful chemical tool at the last stage of the synthesis of kinase inhibitors allowed the synthesis of arrays of molecules inspired by fragment-growing studies generated by molecular modeling calculations. Among the potentially active compounds designed through this strategy, FC162 (4c) exhibits nanomolar IC50 values against some kinases, and is the best candidate for the development as a DYRK kinase inhibitor.
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