|
rdf:type |
|
|
lifeskim:mentions |
|
|
pubmed:issue |
11
|
|
pubmed:dateCreated |
2003-5-16
|
|
pubmed:abstractText |
A series of 1-benzoyl isoquinolines, based on compound 1, was synthesized and evaluated for their ability to displace IGF-I from its complex with IGF-binding protein-3. Successful modifications of 1 included the replacement of the 3,4-dihydroxybenzoyl group with a substituted benzyl group. These alternations culminated in the discovery of compounds such as 7o which had excellent in vitro potency (K(i)=9.4 nM) but with one less of the labile catechol functionality of 1.
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Jun
|
|
pubmed:issn |
0960-894X
|
|
pubmed:author |
pubmed-author:ConnorsPatrickP,
pubmed-author:GrossRaymondR,
pubmed-author:GrossTimothyT,
pubmed-author:HuangCharles QCQ,
pubmed-author:LingNicholasN,
pubmed-author:McCarthyJames RJR,
pubmed-author:StrackNathalieN,
pubmed-author:WilcoxenKeithK,
pubmed-author:XXX,
pubmed-author:YewP RPR,
pubmed-author:ZhuYun-FeiYF
|
|
pubmed:issnType |
Print
|
|
pubmed:day |
2
|
|
pubmed:volume |
13
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
1927-30
|
|
pubmed:dateRevised |
2004-11-17
|
|
pubmed:meshHeading |
|
|
pubmed:year |
2003
|
|
pubmed:articleTitle |
6,7-dihydroxyisoquinoline-3-carboxylic acids are potent inhibitors on the binding of insulin-like growth factor (IGF) to IGF-binding proteins: optimization of the 1-position benzoyl side chain.
|
|
pubmed:affiliation |
Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 10555 Science Center Drive, San Diego, CA 92121, USA.
|
|
pubmed:publicationType |
Journal Article
|
