Synthesis and Antileukemic Activity of Chymotrypsin-Activated Derivatives of 3'-Amino-2', 3'-dideoxycytidine. (Synthetic Nucleosides and Nucleotides, XXXIII)

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概要

• 論文の詳細を見る

• 3'-Amino-2', 3'-dideoxycytidine (8) was directly synthesized from 2'-deoxycytidine. 2', 3'-Dideoxy-3'-(N-acyl-L-phenylalanylamino)cytidines (acyl=butoxycarbonyl (9a), acetyl (9b), benzoyl (9c), and n-hexanoyl (9d)) were synthesized as chymotrypsin-activated prodrugs of 8. This N-protection was required for activation by chymotrypsin to 8. In vitro, compound 8 showed high cytotoxic activity against P388 cells, but the prodrugs 9a-d were ineffective. In vivo, however, these prodrugs showed much higher activity than 8 in mice bearing P388 cells.

• 社団法人日本薬学会の論文
• 1995-03-15

著者

• 山口 十四文

  帝京科学大・バイオ

• 実吉 峯郎

  帝京科学大・バイオ

• 川口 健夫

  城西大学薬学部

• 実吉 峯郎

  帝京科学大学バイオサイエンス学科

• 実吉 峯郎

  Department of Biological Sciences, The Nishi-Tokyo University

• 木村 茂

  Faculty of Pharmaceutical Sciences, Hokkaido Univerisity

• 山口 十四文

  Department of Biological Sciences, The Nishi-Tokyo University

• 川口 健夫

  Faculty of Pharmaceutical Sciences, Josai University

• 坂入 宏

  Faculty of Pharmaceutical Sciences, Josai University

• 川口 健夫

  Faculty Of Pharmaceutical Sciences Josai University

• 川口 健夫

  城西大学

• 木村 茂

  Kansai Univ. Osaka Jpn

• 坂入 宏

  Faculty Of Pharmaceutical Sciences Josai University

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