Literature DB >> 10741557

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

G R Brown1, A M Bamford, J Bowyer, D S James, N Rankine, E Tang, V Torr, E J Culbert.   

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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Year:  2000        PMID： 10741557     DOI： 10.1016/s0960-894x(00)00051-2

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  13 in total

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