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Naphthyl ketones: a new class of Janus kinase 3 inhibitors
G R Brown1, A M Bamford, J Bowyer
1Respiratory & Inflammation Research, AstraZeneca, Macclesfield, Cheshire, UK. george.r.brown@astrazeneca.com
Bioorganic & Medicinal Chemistry Letters
|March 31, 2000
Abstract:
Potent inhibition of Janus kinase 3 was found for a series of naphthyl(beta-aminoethyl)ketones (e.g. 7, pIC50 = 7.1+/-0.3). Further studies indicated that these compounds fragment in less than 1 h by retro-Michael reaction in the Jak3 in vitro ELISA assay procedure. The breakdown product of 7, 2-naphthylvinyl ketone (22, pIC50 = 6.8+/-0.3) showed very similar inhibitory activity to 7. Compounds 7 (in neutral buffer) and 22 will be useful pharmacological tools for the investigation of the Janus tyrosine kinase Jak3.