5'-[2-(2-Nitrophenyl)-2-methylpropionyl]-2'-deoxy-5-fluorouridine as a potential bioreductively activated prodrug of FUDR: synthesis, stability and reductive activation.
5'-[2-(2-Nitrophenyl)-2-methylpropionyl]-2'-deoxy-5-fluorouridine was synthesized as a potential bioreductively activated prodrug of 5-fluoro-2'-deoxyuridine (FUDR). The target compound was stable in both phosphate buffer and human serum and was found to release quickly the parent drug FUDR in quantitative yield upon mild chemical reduction.
Hu
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L
Department of Pharmaceutical Chemistry, College of Pharmacy, Rutgers, The State University of New Jersey, Piscataway 08854, USA. longhu@rci.rutgers.edu
Liu
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B
Hacking
D R
DR
D001682:Biological Availability; D001711:Biotransformation; D004355:Drug Stability; D005467:Floxuridine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics*; D006801:Humans; D010084:Oxidation-Reduction; D011355:Prodrugs / Q000493:pharmacokinetics*
C409453:5'-(2-(2-Nitrophenyl)-2-methylpropionyl)-2'-deoxy-5-fluorouridine; D011355:Prodrugs; D005467:Floxuridine