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Discovery of pyrido[3,4-g]quinazoline derivatives as CMGC family protein kinase inhibitors: Design, synthesis, inhibitory potency and X-ray co–crystal structure

Abstract:
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.
Publication status:
Published
Peer review status:
Peer reviewed
Version:
Accepted Manuscript

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Publisher copy:
10.1016/j.ejmech.2016.04.004

Authors


Zeinyeh, W More by this author
Boibessot, T More by this author
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Publisher:
Elsevier Publisher's website
Journal:
European Journal of Medicinal Chemistry Journal website
Volume:
118
Pages:
170-177
Publication date:
2016-04-05
DOI:
EISSN:
1768-3254
ISSN:
0223-5234
URN:
uuid:b4a00d35-e9aa-442e-b5fa-cc3ea2028268
Source identifiers:
619505
Local pid:
pubs:619505

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