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Synthesis of fluorinated brassinosteroids based on alkene cross-metathesis and preliminary biological assessment
B. Eignerová, B. Slavíková, M. Buděšínský, M. Dračínský, B. Klepetářová, E. Šťastná, M. Kotora
Jazyk angličtina Země Spojené státy americké
Typ dokumentu práce podpořená grantem
PubMed
19719120
DOI
10.1021/jm900495f
Knihovny.cz E-zdroje
- MeSH
- alkeny chemie MeSH
- biotest MeSH
- cholestanoly farmakologie MeSH
- krysa rodu rattus MeSH
- lidé MeSH
- nádorové buněčné linie MeSH
- objevování léků MeSH
- potkani Wistar MeSH
- protinádorové látky farmakologie chemická syntéza chemie metabolismus MeSH
- receptory GABA-A metabolismus MeSH
- steroidy heterocyklické farmakologie MeSH
- steroidy chemická syntéza chemie metabolismus farmakologie MeSH
- zvířata MeSH
- Check Tag
- krysa rodu rattus MeSH
- lidé MeSH
- mužské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- práce podpořená grantem MeSH
Three types of brassinosteroid analogues with perfluoroalkylated side chains were synthesized by using alkene cross-metathesis of a brassinosteroid derivative bearing a terminal alkene moiety with different (perfluoroalkyl)propenes. The presence of the double bonds in the cross-metathesis products allowed a facile one-step double dihydroxylation to provide intermediates that after Baeyer-Villiger oxidation afforded the target compounds. Biological activity of the prepared analogues was tested in GABA(A) receptor, cytotoxic, and brassinolide activity, which reached in some cases the same range as their nonfluorinated analogues.
Citace poskytuje Crossref.org
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- $a Three types of brassinosteroid analogues with perfluoroalkylated side chains were synthesized by using alkene cross-metathesis of a brassinosteroid derivative bearing a terminal alkene moiety with different (perfluoroalkyl)propenes. The presence of the double bonds in the cross-metathesis products allowed a facile one-step double dihydroxylation to provide intermediates that after Baeyer-Villiger oxidation afforded the target compounds. Biological activity of the prepared analogues was tested in GABA(A) receptor, cytotoxic, and brassinolide activity, which reached in some cases the same range as their nonfluorinated analogues.
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