Naamidine A is an antagonist of the epidermal growth factor receptor and an in vivo active antitumor agent.
J Med Chem
; 41(20): 3909-11, 1998 Sep 24.
Article
en En
| MEDLINE
| ID: mdl-9748366
ABSTRACT
The known 2-aminoimidazole alkaloid naamidine A (1) was isolated from a Fijian Leucetta sp. sponge as an inhibitor of the epidermal growth factor (EGF) receptor. The compound exhibited potent ability to inhibit the EGF signaling pathway and is more specific for the EGF-mediated mitogenic response than for the insulin-mediated mitogenic response. Evaluation in an A431 xenograft tumor model in athymic mice indicated that naamidine A exhibited at least 85% growth inhibition at the maximal tolerated dose of 25 mg/kg. Preliminary mechanism of action studies indicate that the alkaloid fails to inhibit the binding of EGF to the receptor and has no effect on the catalytic activity of purified c-src tyrosine kinase.
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Colección:
01-internacional
Banco de datos:
MEDLINE
Asunto principal:
Alcaloides
/
Receptores ErbB
/
Imidazoles
/
Antineoplásicos
Tipo de estudio:
Prognostic_studies
Límite:
Animals
Idioma:
En
Revista:
J Med Chem
Asunto de la revista:
QUIMICA
Año:
1998
Tipo del documento:
Article
País de afiliación:
Estados Unidos