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A C-14 labeled Py-Im polyamide localizes to a subcutaneous prostate cancer tumor.
Raskatov, Jevgenij A; Puckett, James W; Dervan, Peter B.
Afiliação
  • Raskatov JA; Division of Chemistry and Chemical Engineering, California Institute of Technology, Pasadena, CA 91125, United States.
  • Puckett JW; Division of Chemistry and Chemical Engineering, California Institute of Technology, Pasadena, CA 91125, United States.
  • Dervan PB; Division of Chemistry and Chemical Engineering, California Institute of Technology, Pasadena, CA 91125, United States. Electronic address: dervan@caltech.edu.
Bioorg Med Chem ; 22(16): 4371-5, 2014 Aug 15.
Article em En | MEDLINE | ID: mdl-24780272
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.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Neoplasias da Próstata / Pirróis / Imidazóis / Nylons Limite: Animals Idioma: En Revista: Bioorg Med Chem Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2014 Tipo de documento: Article País de afiliação: Estados Unidos

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Neoplasias da Próstata / Pirróis / Imidazóis / Nylons Limite: Animals Idioma: En Revista: Bioorg Med Chem Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2014 Tipo de documento: Article País de afiliação: Estados Unidos