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Updated: Apr 6, 2026

Synthetic Methodology for Asymmetric Ferrocene Derived Bio-conjugate Systems via Solid Phase Resin-based Methodology
Published on: March 12, 2015
Activity of aminoferrocene-based prodrugs against prostate cancer
Margot Schikora1, Alexander Reznikov2, Liudmila Chaykovskaya2
1Friedrich-Alexander-University of Erlangen-Nürnberg, Department of Chemistry and Pharmacy, Organic Chemistry Chair II, Henkestr. 42, 91054 Erlangen, Germany.
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.
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