Gamma-lactone-Functionalized antitumoral acetogenins are the most potent inhibitors of mitochondrial complex I.
Bioorg Med Chem Lett
; 11(5): 681-4, 2001 Mar 12.
Article
em En
| MEDLINE
| ID: mdl-11266168
ABSTRACT
To study the relevance of the terminal alpha,beta-unsaturated gamma-methyl-gamma-lactone moiety of the antitumoral acetogenins of Annonaceae for potent mitochondrial complex I inhibition, we have prepared a series of semisynthetic acetogenins with modifications only in this part of the molecule, from the natural rolliniastatin-1 (1) and cherimolin-1 (2). Some of the hydroxylated derivatives (1b, 1d and 1e) in addition to two infrequent natural beta-hydroxy gamma-methyl gamma-lactone acetogenins, laherradurin (3) and itrabin (4), are more potent complex I inhibitors than any other known compounds.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Furanos
/
Lactonas
/
Mitocôndrias Cardíacas
/
NADH NADPH Oxirredutases
/
Antineoplásicos
Limite:
Animals
Idioma:
En
Ano de publicação:
2001
Tipo de documento:
Article