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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
3A
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pubmed:dateCreated |
1999-9-20
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pubmed:abstractText |
Farnesyl residues are found as a lipophilic modification of a number of important proteins. In addition, synthetic farnesyl derivatives display a range of biological effects. We have prepared a series of N-acylaspartates as structural analogs of farnesylpyrophosphate in which the farnesyl residue has been replaced by a number of different aliphatic and aromatic carboxylic acids and the aspartate is used as a pyrophosphate surrogate. The corresponding dimethyl esters of these aspartates were assayed against different tumor cell lines. Several N-acylaspartic acid dimethyl esters carrying an aromatic acyl residue displayed a selective antiproliferative effect against THP-1 cells with GI50 values ranging from 7.6 to 1.3 microM.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:issn |
0250-7005
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
19
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2117-20
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pubmed:dateRevised |
2007-11-15
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pubmed:meshHeading |
pubmed-meshheading:10470158-Acylation,
pubmed-meshheading:10470158-Alkyl and Aryl Transferases,
pubmed-meshheading:10470158-Antineoplastic Agents,
pubmed-meshheading:10470158-Aspartic Acid,
pubmed-meshheading:10470158-Cell Division,
pubmed-meshheading:10470158-Drug Design,
pubmed-meshheading:10470158-Drug Screening Assays, Antitumor,
pubmed-meshheading:10470158-Esters,
pubmed-meshheading:10470158-Farnesyltranstransferase,
pubmed-meshheading:10470158-Growth Inhibitors,
pubmed-meshheading:10470158-Molecular Structure,
pubmed-meshheading:10470158-Neoplasm Proteins,
pubmed-meshheading:10470158-Polyisoprenyl Phosphates,
pubmed-meshheading:10470158-Protein Prenylation,
pubmed-meshheading:10470158-Protein Processing, Post-Translational,
pubmed-meshheading:10470158-Sesquiterpenes,
pubmed-meshheading:10470158-Structure-Activity Relationship,
pubmed-meshheading:10470158-Tumor Cells, Cultured
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pubmed:articleTitle |
Synthesis and antiproliferative activity of N-acylaspartic acid dimethyl esters.
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pubmed:affiliation |
Institut für Pharmazeutische Chemie, Philipps-Universität Marburg, Germany. schlitze@mailer.uni-marburg.de
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pubmed:publicationType |
Journal Article,
Comparative Study
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