RSC Medicinal Chemistry · 2020 · 18 citations · 30 references
MedicineMedicinal ChemistryPharmacologyCancer PharmacologyMolecular OncologyMolecular PharmacologyCovalent Inhibitor DesignEnzyme InhibitionTargeted Cancer TherapyCovalent Enzyme InhibitorsCovalent InhibitorsCovalent Kinase InhibitorsCysteine-targeted InhibitorsIrreversible Covalent InhibitorsKinase InhibitorsProtein Kinase InhibitorsTargeted Covalent Inhibitors
-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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Structural Bioinformatics-Based Design of Selective, Irreversible Kinase Inhibitors
Michael S. Cohen, Chao Zhang, Kevan M. Shokat et al. · Science · 2005 · 508 citations · Full text
Émeline Leproult, Sofía Barluenga, Dino Moras et al. · Journal of Medicinal Chemistry · 2011 · 190 citations · Full text