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5-氟尿嘧啶(5-FU)是一种广谱性的抗肿瘤药物,其主要缺点是脂溶性小,口服吸收困难,毒副作用较大。为此,多年来,对5-FU进行了大量的化学修饰工作。已成功用于临床的5-FU衍生物主要有呋喃啶(FT-207),双呋喃啶(Thf_2-5-FU)、氟尿嘧啶脱氧核苷(FUDR)及卡莫氟(HCFU)等。在前文中,我们报道了1,3-二羟烷基-5-氟尿嘧啶和氨基酸短肽负载的5-氟尿嘧啶的合成及其抗肿瘤活性。
5-Fluorouracil (5-FU) is a broad-spectrum anticancer drug with the main disadvantages of low fat solubility, difficulty in oral absorption and high toxic and side effects. To this end, over the years, 5-FU carried out a large number of chemical modifications. The 5-FU derivatives that have been successfully used clinically are mainly FT-207, Thf_2-5-FU, FUDR and HCFU. In the foregoing, we report the synthesis and antitumor activity of 5-fluorouracil loaded with 1,3-dihydroxyalkyl-5-fluorouracil and amino acid short peptides.