2G01

Pyrazoloquinolones as Novel, Selective JNK1 inhibitors

Summary for 2G01

• Entry DOI: 10.2210/pdb2g01/pdb
• Descriptor: Mitogen-activated protein kinase 8, C-jun-amino-terminal kinase-interacting protein 1, SULFATE ION, ... (4 entities in total)
• Functional Keywords: jnk1, c-jun n-terminal kinase, protein kinase jnk1 inhibitors, transferase
• Biological source: Homo sapiens (human); More
• Cellular location: Cytoplasm : P45983 Q9UQF2
• Total number of polymer chains: 4
• Total formula weight: 89441.95

Authors

Abad-Zapatero, C. (deposition date: 2006-02-10, release date: 2006-04-18, Last modification date: 2023-08-30)

Primary citation

Liu, M.,Xin, Z.,Clampit, J.E.,Wang, S.,Gum, R.J.,Haasch, D.L.,Trevillyan, J.M.,Abad-Zapatero, C.,Fry, E.H.,Sham, H.L.,Liu, G.
Synthesis and SAR of 1,9-dihydro-9-hydroxypyrazolo[3,4-b]quinolin-4-ones as novel, selective c-Jun N-terminal kinase inhibitors.
Bioorg.Med.Chem.Lett., 16:2590-2594, 2006

PubMed 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.

PubMed: 16527482
DOI: 10.1016/j.bmcl.2006.02.046

Experimental method

X-RAY DIFFRACTION (3.5 Å)