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KMID : 0617219930040010012
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Duksung Bulletin Phamaceutical Sciences
1993 Volume.4 No. 1 p.12 ~ p.17
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Synthesis and Antitumor Activity of N＾3-derivatives of 5-Fluorouracil
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Abstract
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In order to find out a proper connecting bridge between 5-fluorouracil(5-FU) and a macromolecule such as a polypeptide, potentially hydrolytic N^1-derivartives of 5-FU have been systhesized and evaluated for their biological activity. When tested with in vitro leukmic L_1210 cells all the obtained derivartives exhibited slightly higher antitumor activity than the parent 5-FU. Among them the N^1-carbamoyl analogue 2 and N^1-acetamido analogue 6b showed 50％ inhibition of the L_1210 cell growth at the concentrations of 5.01×10^-8 M and 1.03×10^-7 M, respectively. When tested against sarcoma 180 tumor cells inoculated into mice, the compounds 2 and 6b exhibited, respectively, 62％ and 54％ inhibition of the solid tumor growth at the 5-time doses of 100 ㎎/㎏/day. Both compounds, N^1-carbamoyl analogue 2 and N^1-acetamido analogue 6b, realeased the parent 5-FU when incubated in the L_1210 cell cultural media for 5 hrs.
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KEYWORD
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