rdf:type |
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lifeskim:mentions |
umls-concept:C0007634,
umls-concept:C0022634,
umls-concept:C0043119,
umls-concept:C0220781,
umls-concept:C0752312,
umls-concept:C1366876,
umls-concept:C1370600,
umls-concept:C1701002,
umls-concept:C1833235,
umls-concept:C1883254,
umls-concept:C1999216,
umls-concept:C2603343
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pubmed:issue |
13
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pubmed:dateCreated |
2008-6-16
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pubmed:abstractText |
5-Aminopyrazol-4-yl ketones are prepared rapidly and efficiently using microwave dielectric heating from beta-ketonitriles by treatment with N,N'-diphenylformamidine followed by heterocyclocondensation by irradiation with a hydrazine. The inhibitory activity of RO3201195 prepared by this methodology was confirmed in hTERT-immortalized HCA2 and WS dermal fibroblasts at 200nM concentration, both by ELISA and immunoblot assay, and displays excellent kinase selectivity for p38alpha MAPK over the related stress-activated kinase JNK.
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pubmed:grant |
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pubmed:language |
eng
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pubmed:journal |
|
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/5-amino-1-(4-fluorophenyl)-4-(3-(2,3...,
http://linkedlifedata.com/resource/pubmed/chemical/BIRB 796,
http://linkedlifedata.com/resource/pubmed/chemical/Enzyme Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Ketones,
http://linkedlifedata.com/resource/pubmed/chemical/MAP Kinase Kinase 4,
http://linkedlifedata.com/resource/pubmed/chemical/Naphthalenes,
http://linkedlifedata.com/resource/pubmed/chemical/Nitriles,
http://linkedlifedata.com/resource/pubmed/chemical/Protein Isoforms,
http://linkedlifedata.com/resource/pubmed/chemical/Pyrazoles,
http://linkedlifedata.com/resource/pubmed/chemical/p38 Mitogen-Activated Protein...
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pubmed:status |
MEDLINE
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pubmed:month |
Jul
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pubmed:issn |
1464-3405
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pubmed:author |
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
18
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3745-8
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:18539026-Cell Line,
pubmed-meshheading:18539026-Chemistry, Pharmaceutical,
pubmed-meshheading:18539026-Enzyme Activation,
pubmed-meshheading:18539026-Enzyme Inhibitors,
pubmed-meshheading:18539026-Humans,
pubmed-meshheading:18539026-Inhibitory Concentration 50,
pubmed-meshheading:18539026-Ketones,
pubmed-meshheading:18539026-MAP Kinase Kinase 4,
pubmed-meshheading:18539026-Microwaves,
pubmed-meshheading:18539026-Models, Chemical,
pubmed-meshheading:18539026-Naphthalenes,
pubmed-meshheading:18539026-Nitriles,
pubmed-meshheading:18539026-Protein Isoforms,
pubmed-meshheading:18539026-Pyrazoles,
pubmed-meshheading:18539026-p38 Mitogen-Activated Protein Kinases
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pubmed:year |
2008
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pubmed:articleTitle |
Microwave-assisted synthesis of 5-aminopyrazol-4-yl ketones and the p38(MAPK) inhibitor RO3201195 for study in Werner syndrome cells.
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pubmed:affiliation |
School of Chemistry, Main Building, Cardiff University, Park Place, Cardiff CF10 3AT, UK. Bagleymc@cardiff.ac.uk
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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