title: Biological evaluation of twenty-eight ferrocenyl tetrasubstituted olefins: cancer cell growth inhibition, ROS production and hemolytic activity.
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.
authors.affiliation: Instituto de Química e Biotecnologia, Universidade Federal de Alagoas, Tabuleiro do Martins, Maceió, AL 57072-970, Brazil.
authors.forename: Alane Cabral
authors.initials: AC
authors.lastname: de Oliveira
authors.forename: Elizabeth A
authors.initials: EA
authors.lastname: Hillard
authors.forename: Pascal
authors.initials: P
authors.lastname: Pigeon
authors.forename: Danilo Damasceno
authors.initials: DD
authors.lastname: Rocha
authors.forename: Felipe A R
authors.initials: FA
authors.lastname: Rodrigues
authors.forename: Raquel C
authors.initials: RC
authors.lastname: Montenegro
authors.forename: Letícia V
authors.initials: LV
authors.lastname: Costa-Lotufo
authors.forename: Marilia O F
authors.initials: MO
authors.lastname: Goulart
authors.forename: Gérard
authors.initials: G
authors.lastname: Jaouen
mesh_terms: D000475:Alkenes / Q000737:chemistry / Q000494:pharmacology*; D002455:Cell Division / Q000187:drug effects*; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D005296:Ferrous Compounds / Q000737:chemistry*; D006461:Hemolysis / Q000187:drug effects*; D006801:Humans; D020128:Inhibitory Concentration 50; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D000075163:Metallocenes; D009369:Neoplasms / Q000378:metabolism / Q000473:pathology*; D017382:Reactive Oxygen Species / Q000378:metabolism*; D013055:Spectrophotometry, Infrared
chemical_list: D000475:Alkenes; D005296:Ferrous Compounds; D000075163:Metallocenes; D017382:Reactive Oxygen Species; C004998:ferrocene