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- W2010935374 abstract "Synthesis of several 5-substituted (2′S)-2′-deoxy-2′-C-methylcytidines (8) and -uridines (6, 11) has been accomplished using radical deoxygenation of the 2′-tert-alcohols via their methyl oxalyl esters as a key reaction. Anti-herpes simplex virus type-1 and -2, and anti-varicella-zoster virus activities of the newly synthesized nucleosides were evaluated. Among them, the 5-iodouracil derivative 6e showed the most potent activity against herpes simplex virus type-1, with an EC50 of 0.14 μg/mL without showing cytotoxicity up to 100 μg/mL, but had a weak activity against herpes simplex virus type-2 and no activity against varicella-zoster virus up to 50 μg/mL in vitro. Although the 5-fluorocytosine derivative 8b had a potent anti-herpes simplex virus type-1 activity (EC50 = 0.22 μg/mL), it was rather cytotoxic to the CCRF-HSB-2 human T-cell line (IC50 ≥ 1.0 μg/mL)." @default.
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- W2010935374 date "1996-01-01" @default.
- W2010935374 modified "2023-09-24" @default.
- W2010935374 title "Nucleosides and Nucleotides, Part 144 Synthesis and Antiviral Activity of 5-Substituted (2′S)-2′-Deoxy-2′-C-Methylcytidines and -uridines[1]" @default.
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- W2010935374 doi "https://doi.org/10.1002/ardp.19963290203" @default.
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