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, Mark W. Richards, Sivaprakasam Mangaleswaran, David M. Turner, Roger J. Griffin, Bernard T. Golding, Céline Cano
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.
Topics & Concepts
KinaseCysteineEnzymeCovalent bondChemistryBiochemistryCancer researchMedicineOrganic chemistryClick Chemistry and ApplicationsPeptidase Inhibition and AnalysisHIV/AIDS drug development and treatment