Naphthyl ketones: a new class of Janus kinase 3 inhibitors
…, AM Bamford, J Bowyer, DS James, N Rankine…
文献索引：Brown, George R.; Bamford, Andrea M.; Bowyer, Jonathan; James, Daniel S.; Rankine, Neil; Tang, Eric; Torr, Vanessa; Culbert, Eric J. Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 6 p. 575 - 579
Potent inhibition of Janus kinase 3 was found for a series of naphthyl (β-aminoethyl) ketones (eg 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 ...
