YAKHAK HOEJI (약학회지)

The Pharmaceutical Society of Korea (대한약학회)
권호 표지

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 (Duksung Women's University Research Institute for Pharmaceutical Science) ;
  • Chang, Pan-Sup (Duksung Women's University Research Institute for Pharmaceutical Science) ;
  • Kim, Jae-Wan (Duksung Women's University Research Institute for Pharmaceutical Science) ;
  • Jung, Ki-Hwa (Duksung Women's University Research Institute for Pharmaceutical Science) ;
  • Shin, Soon-Hee (Duksung Women's University Research Institute for Pharmaceutical Science) ;
  • Shin, Hae-Soon (Duksung Women's University Research Institute for Pharmaceutical Science) ;
  • Jung, Soon-Bog (Duksung Women's University Research Institute for Pharmaceutical Science)
  • 이희주 (덕성여자대학교 의약자원 개발연구소) ;
  • 장판섭 (덕성여자대학교 의약자원 개발연구소) ;
  • 김재완 (덕성여자대학교 의약자원 개발연구소) ;
  • 정기화 (덕성여자대학교 의약자원 개발연구소) ;
  • 신순희 (덕성여자대학교 의약자원 개발연구소) ;
  • 신혜순 (덕성여자대학교 의약자원 개발연구소) ;
  • 정순복 (덕성여자대학교 의약자원 개발연구소)
  • Published : 1990.12.28
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Abstract

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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