Preparation and evaluation of [125I]troxacitabine: L -nucleoside model of a potential agent for tumor diagnosis and radiotherapy

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In this study, the optimization of troxacitabine labeling with iodine-125 and its biological evaluation were described. Troxacitabine was labeled via direct electrophilic substitution using chloramine-T as oxidizing agent. The optimum amounts of reactants were: 50μg troxacitabine, 75μg Chloramine-T and ∼19kBq carrier free Na125I. The labeled troxacitabine was stable for more than 24h. Results of the in-vivo evaluation revealed that the new tracer, [125I]troxacitabine, tends to localize in tissues with high proliferation rate with preferential accumulation in cancerous tissues. Imaging should be carried at 3h postinjection. The in vitro cell growth inhibition assay showed that the effect of [125I]troxacitabine was stronger than the effect of cold troxacitabine, which strongly suggested that its cytotoxicity was mainly due to radiotoxicity rather than chemotherapeutic activity. The binding assay revealed that [125I]troxacitabine uptake by the Ehrlich and the ARAC8C cells was high and that it bounded well to DNA. Copyright © 2010 John Wiley & Sons, Ltd.

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