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
- 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
- 조남현; 김정영; 엘가말; 최원경; 박진헌; 김은정; 조정혁; 하현준; 최태현; 오창현
- HSV1-tk; nucleoside; hexitol; iodouracil; MCA-tk; MCA; iodine-125; imaging agents
- Issue Date
- Journal of labelled compounds & radiopharmaceuticals
- VOL 54, NO 2, 93-97
- 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.
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