Activity of aminoferrocene-based prodrugs against prostate cancer

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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