Source:http://linkedlifedata.com/resource/pubmed/id/17600705
Switch to
| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
15
|
| pubmed:dateCreated |
2007-7-10
|
| pubmed:abstractText |
2,4-Dianilino pyrimidines are well-known inhibitors of tyrosine kinases including lymphocyte specific kinase (Lck). Structure-activity relationships at the 4-position are discussed and rationalised. Examples bearing a 2-methyl-5-hydroxyaniline substituent at the 4-position were especially potent but showed poor oral pharmacokinetics. Replacement of this substituent by 4-amino(5-methyl-1H-indazole) yielded compounds with comparable enzyme potency and improved pharmacokinetic properties.
|
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical | |
| pubmed:status |
MEDLINE
|
| pubmed:month |
Aug
|
| pubmed:issn |
0960-894X
|
| pubmed:author |
pubmed-author:AngellRichard MRM,
pubmed-author:BamboroughPaulP,
pubmed-author:BhamraInderI,
pubmed-author:BrownDavidD,
pubmed-author:ChristopherJohn AJA,
pubmed-author:CooperAnthony W JAW,
pubmed-author:FazalLynsey HLH,
pubmed-author:GiordanoIlariaI,
pubmed-author:HindLucyL,
pubmed-author:LeiteP FPF,
pubmed-author:PatelVipulkumar KVK,
pubmed-author:RanshawLisa ELE,
pubmed-author:SimsMartin JMJ,
pubmed-author:SkonePhilip APA,
pubmed-author:SmithKathryn JKJ,
pubmed-author:VickerstaffEmmaE,
pubmed-author:WashingtonMelanieM
|
| pubmed:issnType |
Print
|
| pubmed:day |
1
|
| pubmed:volume |
17
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
4363-8
|
| pubmed:dateRevised |
2009-11-19
|
| pubmed:meshHeading | |
| pubmed:year |
2007
|
| pubmed:articleTitle |
N-4-Pyrimidinyl-1H-indazol-4-amine inhibitors of Lck: indazoles as phenol isosteres with improved pharmacokinetics.
|
| pubmed:affiliation |
GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, UK. Paul.A.Bamborough@gsk.com
|
| pubmed:publicationType |
Journal Article
|