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Anticancer Res ; 30(4): 1243-9, 2010 Apr.
Article in English | MEDLINE | ID: mdl-20530435

ABSTRACT

Toremifene (TOR) has been used as an anti-oestrogen drug for the treatment and prevention of human breast cancer. The aim of this study was the addition of the hydrophilic groups diethylenetriamine pentaacetic acid (DTPA) and glucuronic acid to the starting substance TOR and to label it with technetium-99m ((99m)Tc) radionuclide and to investigate radiopharmaceutical potential of the new compound. The synthesis reactions are completed in four steps, including enzymatic reaction, with the following substeps; preparation of microsomal fraction from Hutu 80 cell line and subsequent purification of UDP-glucuronyl transferase (UDPGT), estimation of protein quantity in microsomal samples and glucuronidation reaction. The results indicate that (99m)Tc-TOR-G may be proposed as a new anti-oestrogen glucuronide imaging agent for ovarian tumours.


Subject(s)
Estrogen Receptor Modulators/chemical synthesis , Organotechnetium Compounds/chemical synthesis , Radiopharmaceuticals/chemical synthesis , Technetium Compounds/chemical synthesis , Toremifene/analogs & derivatives , Animals , Cell Line, Tumor , Duodenal Neoplasms/diagnostic imaging , Duodenal Neoplasms/metabolism , Estrogen Receptor Modulators/blood , Estrogen Receptor Modulators/chemistry , Estrogen Receptor Modulators/pharmacokinetics , Female , Glucuronic Acid/chemistry , Humans , Isotope Labeling/methods , Muscles/diagnostic imaging , Muscles/metabolism , Organotechnetium Compounds/blood , Organotechnetium Compounds/pharmacokinetics , Ovary/diagnostic imaging , Ovary/metabolism , Pentetic Acid/chemistry , Radionuclide Imaging , Radiopharmaceuticals/blood , Radiopharmaceuticals/pharmacokinetics , Rats , Rats, Wistar , Technetium Compounds/blood , Technetium Compounds/chemistry , Technetium Compounds/pharmacokinetics , Tissue Distribution , Toremifene/chemistry
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