2g01

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Template:STRUCTURE 2g01

Pyrazoloquinolones as Novel, Selective JNK1 inhibitors


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.

About this Structure

2G01 is a Protein complex structure of sequences from Homo sapiens. 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 Page seeded by OCA on Sun May 4 04:31:42 2008

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