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Eur J Med Chem ; 46(9): 3778-87, 2011 Sep.
Article in English | MEDLINE | ID: mdl-21696865

ABSTRACT

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.


Subject(s)
Alkenes/pharmacology , Cell Division/drug effects , Ferrous Compounds/chemistry , Hemolysis/drug effects , Neoplasms/pathology , Reactive Oxygen Species/metabolism , Alkenes/chemistry , Cell Line, Tumor , Drug Screening Assays, Antitumor , Humans , Inhibitory Concentration 50 , Magnetic Resonance Spectroscopy , Mass Spectrometry , Metallocenes , Neoplasms/metabolism , Spectrophotometry, Infrared
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