4.5 Article

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

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 26, Issue 17, Pages 4327-4329

Publisher

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

Funding

  1. Auvergne Region (Jeune Chercheur Program)
  2. French Ministry of Higher Education and Research
  3. 'Fonds Unique Interministeriel' TRIAD project
  4. Fondation Jerome Lejeune
  5. 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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