| Literature DB >> 24780272 |
Jevgenij A Raskatov1, James W Puckett1, Peter B Dervan2.
Abstract
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.Entities:
Keywords: Accumulation; C-14 radiolabeling; Chemotherapy; DNA binding; Small molecule
Mesh:
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Year: 2014 PMID: 24780272 PMCID: PMC4134956 DOI: 10.1016/j.bmc.2014.04.010
Source DB: PubMed Journal: Bioorg Med Chem ISSN: 0968-0896 Impact factor: 3.641