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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Библиографические подробности
Опубликовано в: :RSC Med Chem
Главные авторы: 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
Формат: Artigo
Язык:Inglês
Опубликовано: Royal Society of Chemistry 2020
Предметы:
Chemistry
Online-ссылка: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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