Linked Life Data

19666221

Source:http://linkedlifedata.com/resource/pubmed/id/19666221

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
18
pubmed:dateCreated
2009-8-26
pubmed:abstractText
Mimetics of the C-terminal CAAX tetrapeptide of Ras protein were designed replacing cysteine (C) by 2-hydroxymethylbenzodioxane or 2-aminomethylbenzodioxane, respectively etherified and amidified with 2'-methyl or 2'-methoxy substituted 2-carboxy-4-hydroxybiphenyl and 2,4-dicarboxybiphenyl. These pluri-substituted biphenyl systems, used as internal spacer and AA dipeptide bioisoster, were linked to the methyl ester of l-methionine, glycine or l-leucine by an amide bond. The resultant twelve pairs of stereoisomers at the dioxane C-2 were tested for antiproliferative effect finding the maximum activity for derivatives with methyleneoxy linker between benzodioxane and 2'-methylbiphenyl. Of these compounds, the one with terminal methionine and S configuration proved a good Ras prenylation inhibitor in a cell-based assay.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Sep
pubmed:issn
1464-3405
pubmed:author
pubmed:issnType
Electronic
pubmed:day
15
pubmed:volume
19
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
5500-4
pubmed:meshHeading
pubmed:year
2009
pubmed:articleTitle
New Ras CAAX mimetics: design, synthesis, antiproliferative activity, and RAS prenylation inhibition.
pubmed:affiliation
Dipartimento di Scienze Farmaceutiche 'Pietro Pratesi', Università degli Studi di Milano, via Mangiagalli 25, I-20133 Milano, Italy.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't