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Studies of the pharmacokinetics and toxicology of 2,3-dideoxy-beta-L-5-fluorocytidine and 2,3-dideoxy-beta-L-cytidine in vivo; and synthesis and antiviral evaluations of 2,3-dideoxy-beta-L-5-azacytidine



Studies of the pharmacokinetics and toxicology of 2,3-dideoxy-beta-L-5-fluorocytidine and 2,3-dideoxy-beta-L-cytidine in vivo; and synthesis and antiviral evaluations of 2,3-dideoxy-beta-L-5-azacytidine



Nucleosides & Nucleotides 14(3-5): 619-625



The pharmacokinetics and toxicology of 2',3'-dideoxy-beta-L-5-fluorocytidine (beta-L-FddC) and 2',3'-dideoxy-beta-L-cytidine (beta-L-ddC) in mice was investigated. In addition, 2',3'-dideoxy-beta-L-5-azacytidine (beta-L-5-aza-ddC) and its alpha-L-anomer (alpha-L-5-azaddC) were synthesized by coupling the silylated 5-azacytosine derivative with 1-O-acetyl-5-O-(tert-butyldimethylsilyl)-2,3-dideoxy-L-ribofuranose, followed by separation of the alpha- and beta-anomers and were evaluated in vitro against HBV and HIV. beta-L-5-aza-ddC was found to show significant anti-HBV activity at approximately the same level as 2',3'-dideoxy-beta-D-cytidine (ddC), which is a known anti-HBV agent. beta-L-5-aza-ddC was not cytotoxic to L1210, P388, S-180, and CCRF-CEM cells up to a concentration of 100 mu-M. Conversely, the alpha-L-anomer was not active against HBV at the same concentration.

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