Title of article :
Synthesis and SAR of 1,9-dihydro-9-hydroxypyrazolo[3,4-b]quinolin-4-ones as novel, selective c-Jun N-terminal kinase inhibitors
Author/Authors :
Mei Liu، نويسنده , , Zhili Xin، نويسنده , , Jill E. Clampit، نويسنده , , Sanyi Wang، نويسنده , , Rebecca J. Gum، نويسنده , , Deanna L. Haasch، نويسنده , , James M. Trevillyan، نويسنده , , Cele Abad-Zapatero، نويسنده , , Elizabeth H. Fry، نويسنده , , Hing L. Sham، نويسنده , , Gang Liu، نويسنده ,
Abstract :
A novel class of 1,9-dihydro-9-hydroxypyrazolo[3,4-b]quinolin-4-ones as c-Jun-N-terminal kinase (JNK) inhibitors is described. These compounds were synthesized via the condensation of 2-nitrobenzaldehydes and hydroxypyrazoles. The structure–activity relationships (SAR) and kinase selectivity profile of the inhibitors are also discussed. Compound 16 was identified as a potent JNK inhibitor with good cellular potency.
Keywords :
JNK , Diabetes , obesity , Pyrazoloquinolinones
