2-Arylamino-6-ethynylpurines are cysteine-targeting irreversible inhibitors of Nek2 kinase

Renewed interest in covalent inhibitors of enzymes implicated in disease states has afforded several agents targeted at protein kinases of relevance to cancers. We now report the design, synthesis and biological evaluation of 6-ethynylpurines that act as covalent inhibitors of Nek2 by capturing a cy...

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Bibliographic Details
Published in:RSC Med Chem
Main Authors: Matheson, Christopher J., Coxon, Christopher R., Bayliss, Richard, Boxall, Kathy, Carbain, Benoit, Fry, Andrew M., Hardcastle, Ian R., Harnor, Suzannah J., Mas-Droux, Corine, Newell, David R., Richards, Mark W., Sivaprakasam, Mangaleswaran, Turner, David, Griffin, Roger J., Golding, Bernard T., Cano, Céline
Format: Artigo
Language:Inglês
Published: Royal Society of Chemistry 2020
Subjects:
Chemistry
Online Access:https://ncbi.nlm.nih.gov/pmc/articles/PMC7649933/
https://ncbi.nlm.nih.gov/pubmed/33479670
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1039/d0md00074d
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