期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 118, 期 -, 页码 170-177出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2016.04.004
关键词
Pyrido[3,4-g]quinazoline; Kinase inhibitors; Ser/Thr kinases; CMGC family; CLK1 binding mode
资金
- Auvergne Region (Jeune Chercheur Program)
- French Ministry of Higher Education and Research
- 'Fonds Unique Interministeriel TRIAD project
- Fondation Jerome Lejeune
- EEC FP7 grant BLUEGENICS
The design and synthesis of new pyrido[3,4-g]quinazoline derivatives is described as well as their protein kinase inhibitory potencies toward five CMGC family members (CDK5, CK1, GSK3, CLK1 and DYRK1A). The interest for this original tricyclic heteroaromatic scaffold as modulators of CLK1/DYRK1A activity was validated by nanomolar potencies (compounds 12 and 13). CLK1 co-crystal structures with two inhibitors revealed the binding mode of these compounds within the ATP-binding pocket. (C) 2016 Elsevier Masson SAS. All rights reserved.
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