Influence of esterification and modification of A-ring in a group of lupane acids on their cytotoxicity
Language English Country Great Britain, England Media print
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
16087342
DOI
10.1016/j.bmc.2005.07.011
PII: S0968-0896(05)00608-5
Knihovny.cz E-resources
- MeSH
- Esterification MeSH
- Carboxylic Acids chemical synthesis pharmacology MeSH
- Humans MeSH
- Molecular Conformation MeSH
- Cell Line, Tumor MeSH
- Cell Proliferation drug effects MeSH
- Drug Screening Assays, Antitumor MeSH
- Triterpenes chemical synthesis pharmacology MeSH
- Dose-Response Relationship, Drug MeSH
- Structure-Activity Relationship MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- Carboxylic Acids MeSH
- lupane MeSH Browser
- Triterpenes MeSH
The aim of this work was to find an optimal ester group for preparation of lupane derivatives connecting high cytotoxicity with good chemical and pharmacological properties. Activities of methyl-, pivaloyloxymethyl- (Pom-), and acetoxymethyl- (Acm-) esters were compared with the activity of free acids. Although the methyl- and Pom-esters were generally less active than free acids, some Acm-esters had cytotoxicity similar to or even better than the starting compounds. Cytotoxic activity was measured in five cancer cell lines.
References provided by Crossref.org
Biocatalysis in the Chemistry of Lupane Triterpenoids