Synthesis and Biological Activity of O-Alkyl-3-N-aminoacyloxymethyl-5-fluoro-2'-deoxyuridine Derivatives

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概要

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• In an attempt to improve the effectiveness of action of 5-fluoro-2'-deoxyuridine (FUdR), various kinds of O-alkylated water-soluble analogues were synthesized. Antitumor activities against sarcoma 180 (solid) were also evaluated. Some compounds exhibited potent activities. In particular, 3'-O-p-chlorobenzyl-3-N-aminoacyloxy-methylester derivatives were effective over a very wide range of dose and gave extremely large therapeutic ratios compared with known 5-fluorouracil (5-FU) derivatives.

• 公益社団法人日本薬学会の論文
• 1996-06-15

著者

• Harada N

  Lead Optimization Research Laboratory Tanabe Seiyaku Co. Ltd.

• Harada Naoyuki

  Lead Optimization Research Laboratory Tanabe Seiyaku Co. Ltd.

• Ozaki Kiyokazu

  Research Institute Of Drug Safety Setsunan University

• Kawaguchi Takayuki

  Lead Optimization Research Laboratory Tanabe Seiyaku Co. Ltd.

• Tsujihara K

  Discovery Research Laboratory Tanabe Seiyaku Co. Ltd.

• Hongu Mitsuya

  Lead Optimization Research Laboratory Tanabe Seiyaku Co. Ltd.

• Oda Kouji

  Lead Optimization Research Laboratory Tanabe Seiyaku Co. Ltd.

• TSUJIHARA Kenji

  Lead Optimization Research Laboratory, Tanabe Seiyaku Co., Ltd.,

• OHASHI Motoaki

  Lead Optimization Research Laboratory, Tanabe Seiyaku Co., Ltd.,

• HASHIYAMA Tomiki

  Lead Optimization Research Laboratory, Tanabe Seiyaku Co., Ltd.,

• OHOHASHI Motoaki

  Lead Optimization Research Laboratory, Tanabe Seiyaku Co., Ltd.,

• Ohashi M

  Lead Optimization Research Laboratory Tanabe Seiyaku Co. Ltd.

• Ozaki K

  Research Institute Of Drug Safety Setsunan University

• Hashiyama T

  Lead Optimization Research Laboratory Tanabe Seiyaku Co. Ltd.

• Hashiyama Tomiki

  Lead Optimization Research Laboratory Tanabe Seiyaku Co. Ltd.

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