2g01
From Proteopedia
(New page: 200px<br /> <applet load="2g01" size="450" color="white" frame="true" align="right" spinBox="true" caption="2g01, resolution 3.50Å" /> '''Pyrazoloquinolones ...) |
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| - | [[Image:2g01.gif|left|200px]]<br /> | + | [[Image:2g01.gif|left|200px]]<br /><applet load="2g01" size="350" color="white" frame="true" align="right" spinBox="true" |
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caption="2g01, resolution 3.50Å" /> | caption="2g01, resolution 3.50Å" /> | ||
'''Pyrazoloquinolones as Novel, Selective JNK1 inhibitors'''<br /> | '''Pyrazoloquinolones as Novel, Selective JNK1 inhibitors'''<br /> | ||
==Overview== | ==Overview== | ||
| - | A novel class of 1,9-dihydro-9-hydroxypyrazolo[3,4-b]quinolin-4-ones as | + | 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== | ==Disease== | ||
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==About this Structure== | ==About this Structure== | ||
| - | 2G01 is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with SO4 and 73Q as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] Full crystallographic information is available from [http:// | + | 2G01 is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=SO4:'>SO4</scene> and <scene name='pdbligand=73Q:'>73Q</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2G01 OCA]. |
==Reference== | ==Reference== | ||
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[[Category: protein kinase jnk1 inhibitors]] | [[Category: protein kinase jnk1 inhibitors]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:26:53 2008'' |
Revision as of 15:26, 21 February 2008
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Pyrazoloquinolones as Novel, Selective JNK1 inhibitors
Contents |
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 and 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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