RESUMO
Several aldehydes related to methyl 9-deoxy-9-oxo-alpha-apopicropodophyllate, a selective antitumour agent against the HT-29 colon carcinoma, have been prepared and evaluated for their cytotoxic activities on four neoplastic cell lines (P-388, A-549, HT-29 and MEL-28). All of them lacked the lactone ring but maintained their cytotoxicity at, or under, the microM level.
Assuntos
Aldeídos/síntese química , Aldeídos/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Lignanas/química , Animais , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Estrutura Molecular , Plasmodium falciparum/efeitos dos fármacos , Análise Espectral , Células Tumorais CultivadasRESUMO
The immunosuppressive activity of several lactonic, nonlactonic, and heterocycle-fused cyclolignans has been demonstrated for the first time by use of a T-cell-mediated immune response. Of the compounds tested, 4'-demethyldeoxypodophyllotoxin (8), beta-apopicropodophyllin (6), and the isoxazoline-fused cyclolignan 15 are the most potent with respect to their suppression of activated splenocytes.
Assuntos
Imunossupressores/farmacologia , Lignanas/farmacologia , Animais , Células Cultivadas , Imunossupressores/síntese química , Lignanas/síntese química , Teste de Cultura Mista de Linfócitos , Camundongos , Camundongos Endogâmicos BALB C , Estrutura Molecular , Baço/citologia , Relação Estrutura-Atividade , Linfócitos T/efeitos dos fármacos , Linfócitos T/imunologiaRESUMO
A series of fused pyrazole derivatives of cyclolignans have been prepared through simple chemical routes and evaluated for their cytotoxic activities in culture cells of P-388 murine leukemia, A-549 lung carcinoma and HT-29 colon carcinoma. Despite the lack of the lactone moiety in their structures, they show IC50 values at microM levels.
