Radiosynthesis and in vitro evaluation of 1-(tetrahydro-5-hydroxy-6-(hydroxymethyl)-2H-pyran-3-yl)-5-[125I]iodouracil: A new potential agent for HSV1-tk reporter gene monitoring

Title
Radiosynthesis and in vitro evaluation of 1-(tetrahydro-5-hydroxy-6-(hydroxymethyl)-2H-pyran-3-yl)-5-[125I]iodouracil: A new potential agent for HSV1-tk reporter gene monitoring
Authors
조남현김정영엘가말최원경박진헌김은정조정혁하현준최태현오창현
Keywords
HSV1-tk; nucleoside; hexitol; iodouracil; MCA-tk; MCA; iodine-125; imaging agents
Issue Date
2011-02
Publisher
Journal of labelled compounds & radiopharmaceuticals
Citation
VOL 54, NO 2, 93-97
Abstract
Synthesis, radiolabelling, and in vitro evaluation of a new 125I-labelled iodouracil hexitol nucleoside analogue are reported. The target compound was successfully synthesized by an iodination–destannylation method and then purified by reverse phase HPLC. The radiochemical purity of the product was >99% with decay-corrected yields of 48±3%. In vitro cellular uptake testing was carried out using MCA and MCA-tk cell lines for comparison of compound 1 with [18F]FHBG. The newly synthesized compound 1 showed higher accumulation in herpex simplex virus type 1 thymidine kinase (HSV1-tk) gene expression cell line (MCA-tk cell line) than in the wild type MCA cell line compared with [18F]FHBG. The MCA-tk to MCA cellular uptake ratio for compound 1 was higher than that of [18F]FHBG from 2 h after incubation. The radioiodine-labelled compound 1 (I-125, t1/2 = 59.37 days) has a longer physical half-life than F-18-(t1/2 = 110 min) labelled FHBG. Radioiodinelabelled compound 1 could be used for monitoring gene expression for a long time. The selectivity for MCA-tk cell line makes compound 1 a promising imaging agent for HSV1-tk expression.
URI
http://pubs.kist.re.kr/handle/201004/40679
ISSN
0362-4803
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KIST Publication > Article
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