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  • Title: Formamidinodoxorubicins are more potent than doxorubicin as apoptosis inducers in human breast cancer cells.
    Author: Marczak A, Denel-Bobrowska M, Łukawska M, Oszczapowicz I.
    Journal: Anticancer Res; 2015 Apr; 35(4):1935-40. PubMed ID: 25862845.
    Abstract:
    BACKGROUND/AIM: The ability of five formamidinodoxorubicins to induce apoptosis of MCF-7 breast cancer cells was tested. All these compounds were modified at C-3' and contain a formamidine group (-N=CH-NRR), with the rest of the cyclic secondary amine (HNRR) of a gradually increasing ring size. MATERIALS AND METHODS: Cytotoxicity was assessed using 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. To analyze apoptosis, double staining using fluorescence probes Hoechst 33258/propidium iodide (PI) and annexin V- Fluorescein isothiocyanate/PI was carried-out. Additionally, the TdT-mediated dUTP nick-end labelling test and activity of caspase 3 were determined. RESULTS: The four tested derivatives displayed a significant increase in antiproliferative activity in comparison to doxorubicin. All of the tested derivatives induced caspase-dependent apoptosis of MCF-7 cells. CONCLUSION: DOX-F MOR and DOX-F PAZ analogs are more potent apoptosis inducers than doxorubicin.
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