氨基酸5—氟尿嘧啶酯类衍生物的合成及其抗肿瘤活性研究

用氨基酸作抗癌药物载体以提高对癌细胞选择性的研究引起了人们的浓厚兴趣。在前文中,我们报道了5-氟尿嘧啶乙酰和丙酰氨基酸及其氨基酸的3-(N′-5-氟尿嘧啶基)-丙醇酯的合成及其抗肿瘤试验研究。本文将报道一系列氨基酸(5-氟尿嘧啶-1,3-双丙基)酯盐酸盐的合成及其体外抗肿瘤活性的研究。 合成路线如下:

Synthesis and Antitumor Activity of Amino Acid 5-Fluorouracil-1,3-dipropyl Esters Hydrochloride

Ten amino acid 5-fluorouracil-1,3-dipropyl esters hydrochloride were obtained by the reaction of N-protected salts of amino acid with 1,3-bis(w-bromopropyl)-5-fluorouracil in the DMF and then deprotecting with HCl-MeOH. The structures of these new compounds were characterized by 1H NMR, IR and UV spectra as well as elemental analysis. The antitumor activities of all of the compounds were tested against EAC in vitro, the preliminary results showed that some of the compounds exhibit certain anititumor activity.