摘要
5-氟尿嘧啶(5-fluorouracil,5-FU)是一种阻止肿瘤细胞嘧啶类核苷酸形成的抗代谢药物,其抗肿瘤作用疗效确切并一直作为治疗胃癌、直肠癌、乳腺癌等的首选药物。但5-氟尿嘧啶的半衰期短、选择性较差、骨髓抑制和胃肠道等不良反应限制了其广泛应用。因此,多年来研究者一直致力于探索研究疗效高、毒副作用低的氟尿嘧啶类衍生物,特别是其1位和3位氮原子上取代的氟尿嘧啶衍生物的研究。本文对5-FU的代谢过程以及目前国内外N1,N3氟尿嘧啶衍生物的研究进展进行综述和评论,以期为5-FU进一步的结构修饰提供参考。
5-Fluorouracil（5-FU） is an antimetabolite of the pyrimidine analogue type,which has clear effect and is primarily applied to treat colorectal cancer, stomach cancer, and breast cancer. However, the clinical applications of 5-FU are subjected to great limitations because of its short plasma half-life ,poorly tumor selectivity, bone marrow suppression, intestinal toxicity and so on. Therefore, people have been attempting to develop new prodrugs of 5-FU with high efficiency and low toxicity ,particularly N^1 ,N^3 fluorouracil derivatives. In this paper,the metabolic pathways of 5-FU and the recent development of N^1 ,N^3 fluorouracil derivatives as potent antitumor agents were reviewed and discussed, which could provide references for further modification of 5- FU.
出处
《中国药物化学杂志》
CAS
CSCD
2014年第5期405-411,共7页
Chinese Journal of Medicinal Chemistry
基金
国家自然科学基金项目(21172134)
