A C-14 labeled Py-Im polyamide localizes to a subcutaneous prostate cancer tumor.
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.
Division of Chemistry and Chemical Engineering, California Institute of Technology, Pasadena, CA 91125, United States.
Jevgenij A
JA
Raskatov
Division of Chemistry and Chemical Engineering, California Institute of Technology, Pasadena, CA 91125, United States.
James W
JW
Puckett
Division of Chemistry and Chemical Engineering, California Institute of Technology, Pasadena, CA 91125, United States. Electronic address: dervan@caltech.edu.
Peter B
PB
Dervan
D000818:Animals; D002250:Carbon Radioisotopes / Q000737:chemistry; D064593:Heterografts; D007093:Imidazoles / Q000737:chemistry / Q000378:metabolism / Q000493:pharmacokinetics*; D007279:Injections, Subcutaneous; D008297:Male; D051379:Mice; D015394:Molecular Structure; D009368:Neoplasm Transplantation; D009757:Nylons / Q000737:chemistry / Q000378:metabolism / Q000493:pharmacokinetics*; D011471:Prostatic Neoplasms / Q000378:metabolism* / Q000473:pathology; D011758:Pyrroles / Q000737:chemistry / Q000378:metabolism / Q000493:pharmacokinetics*; D014018:Tissue Distribution
D002250:Carbon Radioisotopes; D007093:Imidazoles; D009757:Nylons; D011758:Pyrroles
Accumulation; C-14 radiolabeling; Chemotherapy; DNA binding; Small molecule