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5-Fluorouracil-지질 결합체 합성 및 in vitro 항암효과 평가

Syntheses of 5-Fluorouracil-Fat Conjugates and Evaluation of Their in vitro Cytotoxic Activity

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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 N1-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 1X10-7M. Only a dicarboxylic acid derivative, 4e, showed over 50% inhibition at the same level.

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