Author/Authors :
George R. Brown، نويسنده , , Andrea M. Bamford، نويسنده , , Jonathan Bowyer، نويسنده , , Daniel S. James، نويسنده , , Neil Rankine، نويسنده , , Eric Tang، نويسنده , , Vanessa Torr، نويسنده , , Eric J. Culbert، نويسنده ,
Abstract :
Potent inhibition of Janus kinase 3 was found for a series of naphthyl(β-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.
