Design, Synthesis, and Biological Evaluation of Levoglucosenone‐Derived Ras Activation Inhibitors

A panel of new potential Ras ligands was generated by decorating a tricyclic levoglucosenone‐derived scaffold with aromatic moieties. Some members of the panel show in vitro inhibitory activity toward the nucleotide exchange process on Ras and are toxic to some human cancer cell lines. A panel of ne...

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Bibliographic Details
Published in:ChemMedChem 2009-04, Vol.4 (4), p.524-528
Main Authors: Müller, Christian, Gomez‐Zurita Frau, Maria Antonia, Ballinari, Dario, Colombo, Sonia, Bitto, Alessandro, Martegani, Enzo, Airoldi, Cristina, van Neuren, Anske Stephanie, Stein, Matthias, Weiser, Jörg, Battistini, Carlo, Peri, Francesco
Format: Article
Language:English
Subjects:
Animals
antitumor agents
Bridged Bicyclo Compounds, Heterocyclic - chemical synthesis
Bridged Bicyclo Compounds, Heterocyclic - chemistry
Bridged Bicyclo Compounds, Heterocyclic - pharmacology
Cell Line
Cell Proliferation - drug effects
cycloaddition
Drug Design
Enzyme Inhibitors - chemical synthesis
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacology
Glucose - analogs & derivatives
Glucose - chemical synthesis
Glucose - chemistry
Glucose - pharmacology
Humans
Magnetic Resonance Spectroscopy
molecular modeling
Molecular Structure
NMR
ras Proteins - antagonists & inhibitors
ras Proteins - metabolism
signal transduction
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Summary:A panel of new potential Ras ligands was generated by decorating a tricyclic levoglucosenone‐derived scaffold with aromatic moieties. Some members of the panel show in vitro inhibitory activity toward the nucleotide exchange process on Ras and are toxic to some human cancer cell lines. A panel of new potential Ras ligands was generated by decorating a tricyclic levoglucosenone‐derived scaffold with aromatic moieties. Some members of the panel show in vitro inhibitory activity toward the nucleotide exchange process on Ras and are toxic to some human cancer cell lines.
ISSN:1860-7179
1860-7187
DOI:10.1002/cmdc.200800416