Synthesis and SAR of 1,9-dihydro-9-hydroxypyrazolo[3,4-b]quinolin-4-ones as novel, selective c-Jun N-terminal kinase inhibitors

This paper describes a novel class of 1,9-dihydro-9-hydroxypyrazolo[3,4-b]quinolin-4-ones as c-Jun-N-terminal kinase (JNK) inhibitors. These compounds were synthesized via the condensation of 2-nitrobenzaldehydes and hydroxylpyrazoles. The structure–activity relationships (SARs) and kinase selectivi...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2006-05, Vol.16 (10), p.2590-2594
Main Authors: Liu, Mei, Xin, Zhili, Clampit, Jill E., Wang, Sanyi, Gum, Rebecca J., Haasch, Deanna L., Trevillyan, James M., Abad-Zapatero, Cele, Fry, Elizabeth H., Sham, Hing L., Liu, Gang
Format: Article
Language:English
Subjects:
Biological and medical sciences
Crystallography, X-Ray
Diabetes
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacology
General and cellular metabolism. Vitamins
JNK
JNK Mitogen-Activated Protein Kinases - antagonists & inhibitors
Medical sciences
Molecular Structure
Obesity
Pharmacology. Drug treatments
Pyrazoloquinolinones
Quinolones - chemistry
Quinolones - pharmacology
Structure-Activity Relationship
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Summary:This paper describes a novel class of 1,9-dihydro-9-hydroxypyrazolo[3,4-b]quinolin-4-ones as c-Jun-N-terminal kinase (JNK) inhibitors. These compounds were synthesized via the condensation of 2-nitrobenzaldehydes and hydroxylpyrazoles. The structure–activity relationships (SARs) and kinase selectivity profile of the inhibitors are also discussed. Compound 16 was identified as a potent JNK inhibitor with good cellular potency. 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2006.02.046