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

作者：Raskatov Jevgenij A; Puckett James W; Dervan Peter B^*

来源：Bioorganic & Medicinal Chemistry, 2014, 22(16): 4371-4375.

DOI：10.1016/j.bmc.2014.04.010

• C-14 radiolabeling
• Small molecule
• DNA binding
• Accumulation
• Chemotherapy

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.

• 出版日期2014-8-15