| 李楠陈曦梁蓉梅江婉雍小兰.5- 氟尿嘧啶靶向衍生物的研究进展[J].,2011,11(13):2581-2583 |
| 5- 氟尿嘧啶靶向衍生物的研究进展 |
| Advances in Research on 5- Fluorouracil Derivativeswith Targeting Activity |
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| DOI： |
| 中文关键词: 5 - 氟尿嘧啶 靶向性 靶向载体 分子修饰 |
| 英文关键词: 5-Fluorouracil Targeting activity Targeting carrier Molecular modification |
| 基金项目: |
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| 中文摘要: |
| 5 - 氟尿嘧啶是目前临床上的一线抗肿瘤药物之一，其抗瘤谱广，为高效抗代谢药物，但其首过代谢明显，毒副作用大，治疗
剂量与中毒剂量接近，且口服吸收不稳定，半衰期短。因此，对5- 氟尿嘧啶进行有效的分子修饰，以克服其缺点，提高其靶向性，最
大程度地发挥其活性作用和减轻毒副作用，已成为当今抗癌药物研究的热点。本文根据不同靶向载体，对近年来国内外各种分子
修饰的5- 氟尿嘧啶靶向衍生物及其抗肿瘤活性研究进行综述。 |
| 英文摘要: |
| 5-Fluorouracil is one of first line antitumor drugs as a highly active antimetabolite clinically now. It has a broad
antitumor spectrum, but it has shown a significant first pass metabolism, serious toxic side effects, a treatment does near toxic dose, an
unstable oral absorption and a shorter half-life. Therefore, the molecular modification of 5-fluorouracil for overcoming its disadvantages,
improving its targeting activity, playing its active role at the most and reducing its toxic and side effects has become a hot point of
research on anticancer drugs. The recent advances in research on varied molecular modifications of 5-fluorouracil derivatives with
targeting activity and their antitumor activities were reviewed, according to different targeting carriers. |
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