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Bioorg Med Chem Lett. 2016 Sep 1;26(17):4327-9. doi: 10.1016/j.bmcl.2016.07.032. Epub 2016 Jul 16.

Synthesis and preliminary in vitro kinase inhibition evaluation of new diversely substituted pyrido[3,4-g]quinazoline derivatives.

Author information

1
Université Clermont Auvergne, Université Blaise Pascal, Institut de Chimie de Clermont-Ferrand, BP 10448, F-63000 Clermont-Ferrand, France; CNRS, UMR 6296, ICCF, F-63178 Aubière, France.
2
ManRos Therapeutics, Centre de Perharidy, 29680 Roscoff, France.
3
Université Clermont Auvergne, Université Blaise Pascal, Institut de Chimie de Clermont-Ferrand, BP 10448, F-63000 Clermont-Ferrand, France; CNRS, UMR 6296, ICCF, F-63178 Aubière, France. Electronic address: Francis.GIRAUD@univ-bpclermont.fr.
4
Université Clermont Auvergne, Université Blaise Pascal, Institut de Chimie de Clermont-Ferrand, BP 10448, F-63000 Clermont-Ferrand, France; CNRS, UMR 6296, ICCF, F-63178 Aubière, France. Electronic address: Pascale.MOREAU@univ-bpclermont.fr.

Abstract

The synthesis of new diversely substituted pyrido[3,4-g]quinazolines is described. The inhibitory potencies of prepared compounds toward a panel of five CMGC protein kinases (CDK5, CLK1, DYRK1A, CK1, GSK3), that are known to play a potential role in Alzheimer's disease, were evaluated. The best overall kinase inhibition profile was found for nitro compound 4 bearing an ethyl group at the 5-position.

KEYWORDS:

CDK5; CK1; CLK1; DYRK1A; GSK3; Protein kinase inhibition; Pyrido[3,4-g]quinazoline

PMID:
27469128
DOI:
10.1016/j.bmcl.2016.07.032
[Indexed for MEDLINE]

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