Synthesis and preliminary in vitro kinase inhibition evaluation of new diversely substituted pyrido[3,4-g]quinazoline derivatives. - Archive ouverte HAL
Article Dans Une Revue Bioorganic and Medicinal Chemistry Letters Année : 2016

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

Wael Zeinyeh
Lionel Nauton
Nadège Loaëc
Laurent Meijer
Vincent Théry
Fabrice Anizon
Pascale Moreau

Résumé

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.

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Chimie
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Dates et versions

hal-01367659 , version 1 (16-09-2016)

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Citer

Wael Zeinyeh, Yannick J. Esvan, Lionel Nauton, Nadège Loaëc, Laurent Meijer, et al.. Synthesis and preliminary in vitro kinase inhibition evaluation of new diversely substituted pyrido[3,4-g]quinazoline derivatives. . Bioorganic and Medicinal Chemistry Letters, 2016, 26, pp.4327-4329. ⟨10.1016/j.bmcl.2016.07.032⟩. ⟨hal-01367659⟩
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