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Platinum(IV) Prodrugs with Haloacetato Ligands in the Axial Positions can Undergo Hydrolysis under Biologically Relevant Conditions

Authors

  • Dr. Ezequiel Wexselblatt,

    1. Institute for Drug Research, School of Pharmacy, The Hebrew University of Jerusalem, Jerusalem, 91120 (Israel)
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  • Dr. Eylon Yavin,

    1. Institute for Drug Research, School of Pharmacy, The Hebrew University of Jerusalem, Jerusalem, 91120 (Israel)
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  • Prof. Dan Gibson

    Corresponding author
    1. Institute for Drug Research, School of Pharmacy, The Hebrew University of Jerusalem, Jerusalem, 91120 (Israel)
    • Institute for Drug Research, School of Pharmacy, The Hebrew University of Jerusalem, Jerusalem, 91120 (Israel)

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  • D.G. acknowledges partial support from the Israel Science Foundation (grant 1332/10).

Abstract

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Losing ligands rapidly: PtIV complexes with haloacetato ligands can hydrolyze rapidly under biological conditions (pH 7 and 37 °C, see scheme) and the rate increases with increasing pH value. Possible mechanisms for this hydrolysis are examined using H218O and ESI-MS analysis.

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