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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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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 10, 期 8, 页码 797-800

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PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0960-894X(00)00108-6

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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. (C) 2000 Elsevier Science Ltd. All rights reserved.

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