• Title/Summary/Keyword: 5-fluorouracil-fat conjugates

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Syntheses of 5-Fluorouracil-Fat Conjugates and Evaluation of Their in vitro Cytotoxic Activity (5-Fluorouracil-지질 결합체 합성 및 in vitro 항암효과 평가)

  • Lee, Hee-Joo;Chang, Pan-Sup;Kim, Jae-Wan;Jung, Ki-Hwa;Shin, Soon-Hee;Shin, Hae-Soon;Jung, Soon-Bog
    • YAKHAK HOEJI
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    • v.34 no.6
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    • pp.395-400
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    • 1990
  • The FU-fat conjugates(4a-e) as a prodrug have been synthesized by condensing various fatty acids(1a-e) via isocyanates(2a-e) as carbamoyl group at $N^1-position$ of 5-fluorouracil and their structures characterized. Preliminary testing for their antitumor effect was carried out on leukemia L1210 cells in culture. Most of them(4a-d) like the parent FU exhibited less than 50% inhibition on grouth of the cultrued cells at the concentration of $1\;{\times\;10^{-7}M$. Only a dicarboxylic acid derivative, 4e, showed over 50% inhibition at the same level.

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