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Synthesis and biological properties of oxazolinodaunorubicin—a new derivative of daunorubicin with a modified daunosamine moiety

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Summary

Oxazolinodaunorubicin, a new daunorubicin derivative with a modified daunosamine moiety, was synthesized. The biological properties of this derivative and the parent daunorubicin were compared. The results showed antiproliferative activity of the derivative with significantly lower toxicity (an LD50 value ca. 20 times higher than that of parent daunorubicin) and an ability to completely overcome the resistance of cancer cells to this drug in vitro. Cardiotoxicity determination using male mice treated with a single dose of 75% of the LD50 value indicated that the cardiotoxicity of new analog was much lower than that of the parent drug. Preliminary results in transplanted murine tumor models revealed that a single-dose injection of the tested compounds exhibited antitumor activity in P388 and L1210 leukemia and 16/C mammary adenocarcinoma bearing mice.

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Authors and Affiliations

  1. Institute of Biotechnology and Antibiotics, Warsaw, Poland

    Malgorzata Lukawska & Irena Oszczapowicz

  2. Institute of Immunology and Experimental Therapy, Wroclaw, Poland

    Joanna Wietrzyk & Adam Opolski

  3. Warsaw University, Warsaw, Poland

    Janusz Oszczapowicz

Authors
  1. Malgorzata Lukawska
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  2. Joanna Wietrzyk
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  3. Adam Opolski
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  4. Janusz Oszczapowicz
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  5. Irena Oszczapowicz
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Corresponding author

Correspondence to Malgorzata Lukawska.

Additional information

Adam Opolski deceased.

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Lukawska, M., Wietrzyk, J., Opolski, A. et al. Synthesis and biological properties of oxazolinodaunorubicin—a new derivative of daunorubicin with a modified daunosamine moiety. Invest New Drugs 28, 600–608 (2010). https://doi.org/10.1007/s10637-009-9299-4

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  • DOI: https://doi.org/10.1007/s10637-009-9299-4

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