5- 氟尿嘧啶靶向衍生物的研究进展

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。

Advances in Research on 5- Fluorouracil Derivatives with Targeting Activity

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.