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El-Ghany, E. A.; Mahdy, Mahmoud A.; Attallah, K. M.; Ghazy, Fakhr-eldin S.

doi:10.1023/a:1015268611569

Cited by 12 publications

(5 citation statements)

References 12 publications

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“…At appropriate time intervals after injection, mice were sacrificed. The organs as well as the other body parts were dissected 2. Activity in each organ was counted and expressed as a percent of the injected activity per organ.…”

Section: Methodsmentioning

confidence: 99%

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

El-Kawy¹,

Hashem²,

Amin³

et al. 2010

Labelled Comp Radiopharmac

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aIn 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: 50 lg troxacitabine, 75 lg Chloramine-T and $19 kBq carrier free Na 125 I. The labeled troxacitabine was stable for more than 24 h. Results of the in-vivo evaluation revealed that the new tracer, [ 125 I]troxacitabine, tends to localize in tissues with high proliferation rate with preferential accumulation in cancerous tissues. Imaging should be carried at 3 h postinjection. The in vitro cell growth inhibition assay showed that the effect of [ 125 I]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 [125 I]troxacitabine uptake by the Ehrlich and the ARAC8C cells was high and that it bounded well to DNA.

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Section: Methodsmentioning

confidence: 99%

“…125 I‐labeled nucleoside analogs, such as deoxyuridine,1 cytarabine2 and gemcitabine3, have attracted the attention as tumor imaging and therapeutic agents. The iodinated compounds behave like thymidine due to the similarity of Van der Waals radii 4.…”

Section: Introductionmentioning

confidence: 99%

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

El-Kawy¹,

Hashem²,

Amin³

et al. 2010

Labelled Comp Radiopharmac

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“…Chloramine-T can be used to assist the reaction, especially if aromatic substitution is involved -the displacement of a boronate group to give a labelled aryl iodide 172 or the iodination of tyrosine, 173 for example. Another standard procedure is the use of 'Iodogen' which has been used recently to prepare [ 125 I]cytarabine 174 and iodine-125 labelled hormones. 175,176 The more sophisticated method of labelling is that of iododestannylation, i.e.…”

Section: And 131 I)mentioning

confidence: 99%

27 Radiochemistry

Urch

2003

Annu. Rep. Prog. Chem., Sect. A: Inorg. Chem.

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Successive bombardment of the same target with different ion beams to build up a tailor-made mixture of isotopes. This enables a single multiple tracer experiment to be carried out rather than tediously preparing and purifying many different isotopes and carrying out many different experiments. (refs. 12 and 30). An electrochemical method for the direct nucleophilic reaction of the [ 18 F]fluoride anion with benzene. (ref. 115). The use of super critical carbon dioxide for the extraction of actinide elements (refs. 250 and 251)

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“…In addition to that the process of 125 I decay by electron capture leaves the resulting daughter nuclide 125 Te with a mean net charge of 18 interfering with the DNA repair process. 2 In contrast, toxicity is minimal when decay occurs on the cell membranes or extracellular sites. 3 Gemcitabine is an antimetabolite nucleoside analogue that exhibits antineoplastic activity.…”

Section: Introductionmentioning

confidence: 99%

Labeling, biodistribution and evaluation of [¹²⁵I] gemcitabine: a potential agent for tumor diagnosis and radiotherapy

El-Kawy¹,

Hashem²,

Amin³

et al. 2009

Labelled Comp Radiopharmac

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aIn this study, the optimization of gemcitabine labeling with iodine-125 and its biological evaluation are described. Gemcitabine was labeled via direct electrophilic substitution using chloramine-T as an oxidizing agent. The optimum amounts of reactants were 75 mg gemcitabine, 75 mg chloramine-T and 18 MBq carrier-free Na 125 I. The labeled gemcitabine was stable for more than 20 h. Results of the in vivo evaluation revealed that the new tracer, [125 I] gemcitabine, tends to localize in tissues with high proliferation rate with preferential accumulation in cancerous tissues. Imaging should be carried at 2-h postinjection. The in vitro cell growth inhibition assay showed that the effect of [ 125 I] gemcitabine was stronger than the effect of tenfold cold gemcitabine, which strongly suggested that its cytotoxicity was mainly due to radiotoxicity rather than chemotherapeutic activity. The binding assay revealed that [125 I] gemcitabine uptake by the Ehrlich cells was high and that it bound well to DNA where the decay of the radionuclide introduced lethal irreversible double-strand breaks.

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Untitled

Cited by 12 publications

References 12 publications

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

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

27 Radiochemistry

Labeling, biodistribution and evaluation of [¹²⁵I] gemcitabine: a potential agent for tumor diagnosis and radiotherapy

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Cited by 12 publications

References 12 publications

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

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

27 Radiochemistry

Labeling, biodistribution and evaluation of [125I] gemcitabine: a potential agent for tumor diagnosis and radiotherapy

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

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

Labeling, biodistribution and evaluation of [¹²⁵I] gemcitabine: a potential agent for tumor diagnosis and radiotherapy