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Molecules 2016, 21(5), 578; doi:10.3390/molecules21050578

Synthesis of Thiazolo[5,4-f]quinazolin-9(8H)-ones as Multi-Target Directed Ligands of Ser/Thr Kinases

1
Normandie Univ; Uni Rouen; INSA; CNRS, COBRA, UMR 6014, 76000 Rouen, France
2
Protein Phosphorylation & Human Disease group, Station Biologique, 29680 Roscoff, France
3
Manros Therapeutics, Centre de Perharidy, 29680 Roscoff, France
*
Author to whom correspondence should be addressed.
Academic Editors: Panayiotis A. Koutentis and Andreas S. Kalogirou
Received: 7 April 2016 / Revised: 22 April 2016 / Accepted: 23 April 2016 / Published: 30 April 2016
(This article belongs to the Special Issue Sulfur-Nitrogen Heteroaromatics)
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Abstract

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. View Full-Text
Keywords: thiazolo[5,4-f]quinazolin-9(8H)-ones; multi-target-directed ligand; protein kinases; microwave-assisted synthesis; CDK5; GSK-3; CLK1; CK1; DYRK1A. thiazolo[5,4-f]quinazolin-9(8H)-ones; multi-target-directed ligand; protein kinases; microwave-assisted synthesis; CDK5; GSK-3; CLK1; CK1; DYRK1A.
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Hédou, D.; Godeau, J.; Loaëc, N.; Meijer, L.; Fruit, C.; Besson, T. Synthesis of Thiazolo[5,4-f]quinazolin-9(8H)-ones as Multi-Target Directed Ligands of Ser/Thr Kinases. Molecules 2016, 21, 578.

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