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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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Autores principales: 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
格式: Online 文件 Texto
语言:English
出版: Royal Society of Chemistry 2020
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在线阅读:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7649933/
https://www.ncbi.nlm.nih.gov/pubmed/33479670
http://dx.doi.org/10.1039/d0md00074d