Source:http://linkedlifedata.com/resource/pubmed/id/21316221
Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
6
|
pubmed:dateCreated |
2011-3-7
|
pubmed:abstractText |
Quinazoline 3 was discovered as a novel c-jun N-terminal kinase (JNK) inhibitor with good brain penetration and pharmacokinetic (PK) properties. A number of analogs which were potent both in the biochemical and cellular assays were discovered. Quinazoline 13a was found to be a potent JNK3 inhibitor (IC(50)=40 nM), with >500-fold selectivity over p38, and had good PK and brain penetration properties. With these properties, 13a is considered a potential candidate for in vivo evaluation.
|
pubmed:grant | |
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical | |
pubmed:status |
MEDLINE
|
pubmed:month |
Mar
|
pubmed:issn |
1464-3405
|
pubmed:author |
pubmed-author:CameronMichael DMD,
pubmed-author:ChenWeiminW,
pubmed-author:DuckettDerekD,
pubmed-author:HeYuanjunY,
pubmed-author:JooFF,
pubmed-author:KameneckaTheodore MTM,
pubmed-author:KhanSusanS,
pubmed-author:KoenigMarcelM,
pubmed-author:LingYuan YuanYY,
pubmed-author:LoGrassoPhilip VPV,
pubmed-author:NoelRomainR,
pubmed-author:RongJiangJ,
pubmed-author:ShinYouseungY,
pubmed-author:SongXinyiX
|
pubmed:copyrightInfo |
Copyright © 2011 Elsevier Ltd. All rights reserved.
|
pubmed:issnType |
Electronic
|
pubmed:day |
15
|
pubmed:volume |
21
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
1719-23
|
pubmed:meshHeading |
pubmed-meshheading:21316221-Brain,
pubmed-meshheading:21316221-Inhibitory Concentration 50,
pubmed-meshheading:21316221-JNK Mitogen-Activated Protein Kinases,
pubmed-meshheading:21316221-Protein Kinase Inhibitors,
pubmed-meshheading:21316221-Quinazolines,
pubmed-meshheading:21316221-Structure-Activity Relationship
|
pubmed:year |
2011
|
pubmed:articleTitle |
Synthesis and SAR of novel quinazolines as potent and brain-penetrant c-jun N-terminal kinase (JNK) inhibitors.
|
pubmed:affiliation |
Department of Molecular Therapeutics and Translational Research Institute, The Scripps Research Institute, Scripps Florida, 130 Scripps Way #A2A, Jupiter, FL 33458, USA.
|
pubmed:publicationType |
Journal Article,
Research Support, N.I.H., Extramural
|