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- W2022041370 abstract "To circumvent the in vivo instability of 5-iodo-2′-deoxyuridine (IUdR), a 2′-fluorine-substituted analogue, 5-iodo-1-(2-deoxy-2-fluoro-β-d-arabinofuranosyl)uracil (FIAU) recently has been introduced. To facilitate the preparation of radioiodinated FIAU as well as its astatinated analogue, a tin precursor, 5-trimethylstannyl-1-(2-deoxy-2-fluoro-β-d-arabinofuranosyl)uracil (FTAU) was synthesized. Both [125/131I]FIAU and 5-[211At]astato-1-(2-deoxy-2-fluoro-β-d-arabinofuranosyl)uracil (FAAU) were prepared from FTAU in more than 85% radiochemical yield under mild conditions. The in vitro serum stability of both fluorine-substituted derivatives was higher than that of the corresponding unsubstituted parents. The enhanced stability of fluorinated derivatives was even more apparent in whole blood. The uptake of [125I]FIAU in D-247 MG human glioma cells in vitro was 20-fold higher than that of [125I]IUdR over an activity concentration range of 5–100 kBq/mL; the uptake of FAAU was not significantly different from that of 5-[211At]astato-2′-deoxyuridine (AUdR). Accumulation of radioiodine in mouse thyroid in vivo with [131I]FIAU was fivefold lower than [125I]IUdR, indicating that the former was less susceptible to deiodination. The tissue uptake of FAAU was similar to that reported for AUdR." @default.
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- W2022041370 date "1991-04-01" @default.
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- W2022041370 title "Antiviral activity of FIAU versus strains of CMV sensitive and resistant to ganciclovir" @default.
- W2022041370 doi "https://doi.org/10.1016/0166-3542(91)90208-9" @default.
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