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Semisynthesis of alpha-methyl-gamma-lactones and in vitro evaluation of their activity on protein farnesyltransferase.
- Source :
-
Journal of enzyme inhibition and medicinal chemistry [J Enzyme Inhib Med Chem] 2010 Apr; Vol. 25 (2), pp. 172-9. - Publication Year :
- 2010
-
Abstract
- The semisynthesis of xanthanolide derivatives is reported from xanthinin and 4-epi-isoxanthanol, two sesquiterpene lactones isolated from the crude chloroformic extract of the leaves of Xanthium macrocarpum DC. (Asteraceae) by liquid/liquid chromatography. In vitro evaluation of their protein farnesyltransferase (PFTase) inhibitory activity has been investigated. In contrast to other biological activities of xanthanolides, PFTase inhibition is not associated with the presence of the potentially toxic alpha-methylene-gamma-lactone function.
- Subjects :
- Colonic Neoplasms drug therapy
Colonic Neoplasms pathology
Enzyme Assays
HCT116 Cells
Humans
Sesquiterpenes chemistry
Solvents chemistry
Alkyl and Aryl Transferases antagonists & inhibitors
Chloroform chemistry
Enzyme Inhibitors chemical synthesis
Enzyme Inhibitors chemistry
Enzyme Inhibitors pharmacology
Lactones chemical synthesis
Lactones chemistry
Lactones pharmacology
Plant Extracts chemistry
Plant Leaves chemistry
Sesquiterpenes chemical synthesis
Sesquiterpenes isolation & purification
Sesquiterpenes pharmacology
Xanthium chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1475-6374
- Volume :
- 25
- Issue :
- 2
- Database :
- MEDLINE
- Journal :
- Journal of enzyme inhibition and medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 20222761
- Full Text :
- https://doi.org/10.3109/14756360903169592