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Critical role of a methyl group on the γ-lactone ring of annonaceous acetogenins in the potent inhibition of mitochondrial complex I
- Source :
- Bioorganicmedicinal chemistry letters. 23(5)
- Publication Year :
- 2012
-
Abstract
- C34-epi and C34-epi-C35-trifluoro analogues of solamin, a mono-THF annonaceous acetogenin, were synthesized. Their inhibitory activity, along with previously synthesized analogues (C35-fluoro, C35-difluoro, and C35-trifluorosolamins), against bovine mitochondrial NADH–ubiquinone oxidoreductase (complex I) was determined. The present study revealed that the methyl group on the γ-lactone moiety is critical to the potent inhibition of complex I by natural acetogenins.
- Subjects :
- Models, Molecular
Acetogenins
Stereochemistry
Clinical Biochemistry
Pharmaceutical Science
Ring (chemistry)
Biochemistry
chemistry.chemical_compound
Lactones
Structure-Activity Relationship
Oxidoreductase
Drug Discovery
Moiety
Structure–activity relationship
Animals
Humans
Molecular Biology
chemistry.chemical_classification
Electron Transport Complex I
Organic Chemistry
Mitochondria
chemistry
Acetogenin
Molecular Medicine
Cattle
Annonaceous Acetogenins
Lactone
Methyl group
Subjects
Details
- ISSN :
- 14643405
- Volume :
- 23
- Issue :
- 5
- Database :
- OpenAIRE
- Journal :
- Bioorganicmedicinal chemistry letters
- Accession number :
- edsair.doi.dedup.....652caaa45e25fef77cd739a502ed1702