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Eur J Med Chem ; 40(1): 69-74, 2005 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-15642411

RESUMO

Six new galactoglycerolipid analogs, in which one or two 4-methylpentanoyl or trans-2-butenoyl groups are linked to the 2-O-beta-D-galactosylglycerol skeleton, were tested for their anti-tumor-promoting activity using a short-term in vitro assay for Epstein-Barr virus early antigen (EBV-EA) activation. All these compounds were more active than their linear or saturated reference compounds in inhibiting the EBV activation promoted by the tumor promoter 12-O-tetradecanoylphorbol-13-acetate (TPA), the diester 1-O-(4-methylpentanoyl)-2-O-[6-O-(4-methylpentanoyl)-beta-D-galactopyranosyl]-sn-glycerol resulting the most active glycoglycerolipid analog till now tested. Four compounds (three butenoates and one 4-methylpentanoate), when tested in the in vivo two-stage carcinogenesis test, exhibited also inhibitory effects on mouse skin tumor promotion.


Assuntos
Antineoplásicos/química , Antineoplásicos/farmacologia , Galactolipídeos/química , Carga Tumoral/efeitos dos fármacos , Animais , Antígenos Virais/efeitos dos fármacos , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Feminino , Galactolipídeos/farmacologia , Humanos , Camundongos , Camundongos Endogâmicos ICR , Mimetismo Molecular , Papiloma/tratamento farmacológico , Papiloma/patologia , Neoplasias Cutâneas/tratamento farmacológico , Neoplasias Cutâneas/patologia , Relação Estrutura-Atividade
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