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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 towardfive 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 ATPbinding pocket.
Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1016/j.ejmech.2016.04.004

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Institution:
University of Oxford
Division:
MSD
Department:
NDM
Sub department:
Structural Genomics Consortium
Role:
Author
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The Auvergne Region More from this funder
French Ministry of Higher Education and Research More from this funder
Seventh Framework Programme More from this funder
Fonds Unique Interministeriel More from this funder
Fondation Jerome Lejeune More from this funder
Publisher:
Elsevier Publisher's website
Journal:
European Journal of Medicinal Chemistry Journal website
Volume:
118
Pages:
170-177
Publication date:
2016-04-01
Acceptance date:
2016-04-02
DOI:
Source identifiers:
624365
Keywords:
Pubs id:
pubs:624365
UUID:
uuid:39494b46-5603-44db-95ff-51679ee07206
Local pid:
pubs:624365
Deposit date:
2016-05-27

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