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Eur J Med Chem ; 46(9): 3778-87, 2011 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-21696865

RESUMO

The antiproliferative effects of twenty-eight tetrasubstituted olefins bearing a ferrocenyl group, including six never-reported compounds, were evaluated against SF-295 (human glioblastoma), HCT-8 (human colon cancer), MDA-MB-435 (human melanoma) and HL-60 (human promyelocytic leukemia) using the MTT test. IC(50) values were determined for twenty-three active compounds and of these, ten compounds had IC(50) values lower than 2 µM on one or more cell lines. Of all the compounds, only two produced significant amounts of ROS on HL-60 cells, and ROS production and growth inhibition could not be correlated. The ten most antiproliferative compounds were tested for their hemolytic activity on mouse erythrocytes. Five compounds showing high antiproliferative activity and low hemolytic activity were thus identified for further study.


Assuntos
Alcenos/farmacologia , Divisão Celular/efeitos dos fármacos , Compostos Ferrosos/química , Hemólise/efeitos dos fármacos , Neoplasias/patologia , Espécies Reativas de Oxigênio/metabolismo , Alcenos/química , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Concentração Inibidora 50 , Espectroscopia de Ressonância Magnética , Espectrometria de Massas , Metalocenos , Neoplasias/metabolismo , Espectrofotometria Infravermelho
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