Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 26, Issue 17, Pages 4327-4329Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2016.07.032
Keywords
Pyrido[3,4-g]quinazoline; Protein kinase inhibition; CLK1; DYRK1A; CDK5; GSK3; CK1
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Funding
- Auvergne Region (Jeune Chercheur Program)
- French Ministry of Higher Education and Research
- 'Fonds Unique Interministeriel' TRIAD project
- Fondation Jerome Lejeune
- EEC FP7 grant BLUEGENICS
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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. (C) 2016 Elsevier Ltd. All rights reserved.
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