• Bioorg. Med. Chem. · Aug 2014

    A C-14 labeled Py-Im polyamide localizes to a subcutaneous prostate cancer tumor.

    • Jevgenij A Raskatov, James W Puckett, and Peter B Dervan.
    • Division of Chemistry and Chemical Engineering, California Institute of Technology, Pasadena, CA 91125, United States.
    • Bioorg. Med. Chem. 2014 Aug 15; 22 (16): 4371-5.

    AbstractIn an effort to quantitate Py-Im polyamide concentrations in vivo, we synthesized the C-14 radioactively labeled compounds 1-3, and investigated their tumor localization in a subcutaneous xenograft model of prostate cancer (LNCaP). Tumor concentrations were compared with representative host tissues, and exhibited a certain degree of preferential localization to the xenograft. Compound accumulation upon repeated administration was measured. Py-Im polyamide 1 was found to accumulate in LNCaP tumors at concentrations similar to the IC50 value for this compound in cell culture experiments. Copyright © 2014. Published by Elsevier Ltd.

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