2g01

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spinqualitylabelsall models 2g01, resolution 3.50Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image

Pyrazoloquinolones as Novel, Selective JNK1 inhibitors

Contents 1 Overview 2 Disease 3 About this Structure 4 Reference

Overview

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.

Disease

Known diseases associated with this structure: Diabetes mellitus, noninsulin-dependent OMIM:[604641]

About this Structure

2G01 is a Protein complex structure of sequences from Homo sapiens with SO4 and 73Q as ligands. Active as Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 Full crystallographic information is available from OCA.

Reference

Synthesis and SAR of 1,9-dihydro-9-hydroxypyrazolo[3,4-b]quinolin-4-ones as novel, selective c-Jun N-terminal kinase inhibitors., Liu M, Xin Z, Clampit JE, Wang S, Gum RJ, Haasch DL, Trevillyan JM, Abad-Zapatero C, Fry EH, Sham HL, Liu G, Bioorg Med Chem Lett. 2006 May 15;16(10):2590-4. Epub 2006 Mar 9. PMID:16527482

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