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- W2055313734 abstract "Several estrogen-tethered platinum(IV) complexes were prepared and characterized by ESI-MS and 1H NMR spectroscopy. Their design was inspired by the observation that estrogen receptor-positive cells exposed to the hormone are sensitized to cisplatin. Intracellular reduction of bis-estrogen-cis-diamminedichloroplatinum(IV), BEPn (where n = 1–5 methylene groups between Pt and estrogen), occurs to afford cisplatin and two equivalents of the linker-modified estrogen. The ability of BEPn to induce overexpression of HMGB1 was established by immunofluorescence microscopy. The cytotoxicity of the compounds was evaluated in ER(+) MCF-7 and ER(−) HCC-1937 human breast cancer cell lines. BEP3 selectively induces overexpression of HMGB1 in MCF-7 cells, compared to HCC-1937 cells, and enhances their sensitivity (IC50 = 2.1 ± 0.4 μM versus 3.7 ± 0.9 μM, respectively) to the compound. The difference in compound activities and the potential of compounds of this class for treating breast and ovarian cancer are discussed." @default.
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- W2055313734 date "2004-04-01" @default.
- W2055313734 modified "2023-09-26" @default.
- W2055313734 title "Synthesis, Characterization, and Cytotoxicity of a Series of Estrogen-Tethered Platinum(IV) Complexes" @default.
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- W2055313734 doi "https://doi.org/10.1016/j.chembiol.2004.03.024" @default.
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