Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 22, Issue 16, Pages 4371-4375Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2014.04.010
Keywords
C-14 radiolabeling; Small molecule; DNA binding; Accumulation; Chemotherapy
Funding
- Alexander von Humboldt foundation
- National Institutes of Health [GM51747, GM27681]
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In 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. (C) 2014 Published by Elsevier Ltd.
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