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
Format: Artikel
Sprache:eng
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Zusammenfassung: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.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(00)00108-6