Inhibitory effects on mitochondrial complex I of semisynthetic mono-Tetrahydrofuran acetogenin derivatives

Modifications in the terminal α,β-unsaturated γ-methyl-γ-lactone moiety or in the alkyl chain that links this terminal γ-lactone with the α,α′-dihydroxylated THF system of the natural mono-tetrahydrofuranic acetogenins, annonacin and annonacinone, led to the preparation of eight semisynthetic deriva...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2003-11, Vol.13 (22), p.4101-4105
Hauptverfasser:	Tormo, José R, Gallardo, Teresa, Peris, Eva, Bermejo, Almudena, Cabedo, Nuria, Estornell, Ernesto, Zafra-Polo, M.Carmen, Cortes, Diego
Format:	Artikel
Sprache:	eng
Schlagworte:	Acetogenins Antineoplastic agents Biological and medical sciences Electron Transport Complex I - antagonists & inhibitors Enzyme Inhibitors - pharmacology Fatty Alcohols - chemical synthesis Fatty Alcohols - pharmacology Furans - chemical synthesis Furans - pharmacology General aspects Kinetics Lactones - chemical synthesis Lactones - pharmacology Medical sciences Multienzyme Complexes - antagonists & inhibitors NADH, NADPH Oxidoreductases - antagonists & inhibitors Pharmacology. Drug treatments
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Zusammenfassung:	Modifications in the terminal α,β-unsaturated γ-methyl-γ-lactone moiety or in the alkyl chain that links this terminal γ-lactone with the α,α′-dihydroxylated THF system of the natural mono-tetrahydrofuranic acetogenins, annonacin and annonacinone, led to the preparation of eight semisynthetic derivatives. Their inhibitory effects on mitochondrial complex I is discussed and compared with that of the classical complex I inhibitor, rotenone. Graphic
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2003.08.045