Source:http://linkedlifedata.com/resource/pubmed/id/15149688
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
12
|
| pubmed:dateCreated |
2004-5-19
|
| pubmed:abstractText |
A novel class of 2,3-dihydro-1,3-dioxo-1H-isoindole-5-carboxylic acids are described as inhibitors of the endo-beta-glucuronidase heparanase. Several of the compounds, for example, 2-[4-propylamino-5-[5-(4-chloro)phenyl-benzoxazol-2-yl]phenyl]-2,3-dihydro-1,3-dioxo-1H-isoindole-5-carboxylic acid (9c), display potent heparanase inhibitory activity (IC(50) 200-500 nM) and have high selectivity (>100-fold) over human beta-glucuronidase. They also show anti-angiogenic effects. Such compounds should serve as useful biological tools and may provide a basis for the design of novel therapeutic agents.
|
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical | |
| pubmed:status |
MEDLINE
|
| pubmed:month |
Jun
|
| pubmed:issn |
0960-894X
|
| pubmed:author |
pubmed-author:BennettJames MJM,
pubmed-author:BuckRichard TRT,
pubmed-author:ColvilleClaire SCS,
pubmed-author:CourtneyStephen MSM,
pubmed-author:HayPhilip APA,
pubmed-author:HircockMargaret LML,
pubmed-author:McKenzieEdward AEA,
pubmed-author:PageMartin JMJ,
pubmed-author:PollardFaye CFC,
pubmed-author:PorterDavid WDW,
pubmed-author:ScopesDavid I CDI,
pubmed-author:StubberfieldColin RCR,
pubmed-author:TurnerPaul RPR
|
| pubmed:issnType |
Print
|
| pubmed:day |
21
|
| pubmed:volume |
14
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
3269-73
|
| pubmed:meshHeading | |
| pubmed:year |
2004
|
| pubmed:articleTitle |
2,3-Dihydro-1,3-dioxo-1H-isoindole-5-carboxylic acid derivatives: a novel class of small molecule heparanase inhibitors.
|
| pubmed:affiliation |
Department of Medicinal Chemistry, Celltech R&D Ltd, 4-10 The Quadrant, Abingdon Science Park, Abingdon, Oxfordshire, OX14 4YS, UK.
|
| pubmed:publicationType |
Journal Article
|