title: Activity of aminoferrocene-based prodrugs against prostate cancer.
abstract: We tested cytotoxicity of aminoferrocene-based prodrugs towards human androgen-responsive and unresponsive prostate cancer cell lines LNCaP and DU-145 correspondingly. Two prodrugs were selected, which are both activated at elevated concentrations of ROS with generation of quinone methide (antioxidant system inhibitor) and iron-containing compounds (N-benzylaminoferrocene (prodrug 1) and Fe salts (2)). We observed that only prodrug 1 is active against the selected prostate cancer cells (IC50=11-27 μM) and its activity correlates with the high cell-membrane permeability and increased production of intracellular ROS.
authors.affiliation: Friedrich-Alexander-University of Erlangen-Nürnberg, Department of Chemistry and Pharmacy, Organic Chemistry Chair II, Henkestr. 42, 91054 Erlangen, Germany.
authors.forename: Margot
authors.initials: M
authors.lastname: Schikora
authors.affiliation: V.P. Komisarenko Institute of Endocrinology and Metabolism, National Academy of Medical Sciences of Ukraine, Kyiv, Ukraine.
authors.forename: Alexander
authors.initials: A
authors.lastname: Reznikov
authors.affiliation: V.P. Komisarenko Institute of Endocrinology and Metabolism, National Academy of Medical Sciences of Ukraine, Kyiv, Ukraine.
authors.forename: Liudmila
authors.initials: L
authors.lastname: Chaykovskaya
authors.affiliation: V.P. Komisarenko Institute of Endocrinology and Metabolism, National Academy of Medical Sciences of Ukraine, Kyiv, Ukraine.
authors.forename: Olga
authors.initials: O
authors.lastname: Sachinska
authors.affiliation: V.P. Komisarenko Institute of Endocrinology and Metabolism, National Academy of Medical Sciences of Ukraine, Kyiv, Ukraine.
authors.forename: Lubov
authors.initials: L
authors.lastname: Polyakova
authors.affiliation: Friedrich-Alexander-University of Erlangen-Nürnberg, Department of Chemistry and Pharmacy, Organic Chemistry Chair II, Henkestr. 42, 91054 Erlangen, Germany. Electronic address: Andriy.Mokhir@fau.de.
authors.forename: Andriy
authors.initials: A
authors.lastname: Mokhir
mesh_terms: D000818:Animals; D017209:Apoptosis; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects*; D005296:Ferrous Compounds / Q000737:chemistry*; D006801:Humans; D008297:Male; D051379:Mice; D011355:Prodrugs / Q000494:pharmacology*; D011471:Prostatic Neoplasms / Q000188:drug therapy*; D017382:Reactive Oxygen Species / Q000378:metabolism
chemical_list: D005296:Ferrous Compounds; D011355:Prodrugs; D017382:Reactive Oxygen Species
keywords: Aminoferrocene; Iron; Prodrug; Prostate cancer; Reactive oxygen species