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 dru...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2000-04, Vol.10 (8), p.797-800
Hauptverfasser: LONGQIN HU, BIN LIU, HACKING, D. R
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container_title Bioorganic & medicinal chemistry letters
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creator LONGQIN HU
BIN LIU
HACKING, D. R
description 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.
doi_str_mv 10.1016/S0960-894X(00)00108-6
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ispartof Bioorganic & medicinal chemistry letters, 2000-04, Vol.10 (8), p.797-800
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language eng
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source MEDLINE; Access via ScienceDirect (Elsevier)
subjects Antineoplastic agents
Biological and medical sciences
Biological Availability
Biotransformation
Drug Stability
Floxuridine - analogs & derivatives
Floxuridine - chemical synthesis
Floxuridine - chemistry
Floxuridine - pharmacokinetics
General aspects
Humans
Medical sciences
Oxidation-Reduction
Pharmacology. Drug treatments
Prodrugs - pharmacokinetics
title 5'-[2-(2-nitrophenyl)-2-methylpropionyl]-2'-deoxy-5-fluorouridine as a potential bioreductively activated prodrug of FUDR: Synthesis, stability and reductive activation
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