6533b831fe1ef96bd129847f
RESEARCH PRODUCT
Epoxy-Acetogenins and other Polyketide Epoxy Derivatives as Inhibitors of the Mitochondrial Respiratory Chain Complex I
M. C. Zafra‐poloDiego CortesErnesto EstornellJosé R. TormoAngel Serranosubject
StereochemistryChemical structurePharmaceutical ScienceEpoxideAnalytical ChemistryElectron TransportLactonesPolyketidechemistry.chemical_compoundDrug DiscoveryNADH NADPH OxidoreductasesMitochondrial respiratory chain complex IFuransMode of actionAlkylPharmacologychemistry.chemical_classificationbiologyOrganic ChemistryEpoxybiology.organism_classificationMitochondriaComplementary and alternative medicinechemistryAnnonaceaevisual_artvisual_art.visual_art_mediumEpoxy CompoundsMolecular Medicinedescription
Annonaceous acetogenins (ACG), an extensive group of cytotoxic natural products, are antitumor agents whose main mode of action is inhibition of the mammalian mitochondrial complex I. Herein we describe the importance of the different chemical groups along the alkyl chain for optimal inhibitory potency, discussing the structurally relevant factors present in these compounds. For this purpose, a series of epoxide derivatives from alpha-linolenic acid were prepared and their activity compared with that of epoxy-acetogenins and tetrahydrofuranic (THF) acetogenins isolated from Rollinia membranacea.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2000-06-24 | Planta Medica |