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

Christopher J. Matheson, Christopher R. Coxon, Richard Bayliss, Kathy Boxall, Benoît Carbain, Andrew M. Fry, Ian R. Hardcastle, Suzannah J. Harnor, Corine Mas-Droux, David R. Newell,

RSC Medicinal Chemistry · 2020 · 18 citations · 30 references

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Abstract

-purin-2-yl)amino)phenyl)acetamide has the attributes of a drug-like compound with good aqueous solubility, no inhibition of hERG at 25 μM and a good stability profile in human liver microsomes. It is concluded that 6-ethynylpurines are promising agents for cancer treatment by virtue of their selective inhibition of Nek2.

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