2. Academic Validation
  3. Naphthyl ketones: a new class of Janus kinase 3 inhibitors

Naphthyl ketones: a new class of Janus kinase 3 inhibitors

  • Bioorg Med Chem Lett. 2000 Mar 20;10(6):575-9. doi: 10.1016/s0960-894x(00)00051-2.
G R Brown 1,  A M Bamford,  J Bowyer,  D S James,  N Rankine,  E Tang,  V Torr,  E J Culbert
Affiliations

Affiliation

  • 1 Respiratory & Inflammation Research, AstraZeneca, Macclesfield, Cheshire, UK. george.r.brown@astrazeneca.com
PMID: 10741557 DOI: 10.1016/s0960-894x(00)00051-2
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.

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