新型L-酪氨酸二肽衍生物的合成及其抗肿瘤活性

以L-酪氨酸甲酯盐酸盐和对羟基苯甲酸（PHBA）为原料，经缩合、水解和亲核取代反应，设计并合成了9个新型的L-酪氨酸二肽衍生物（3b和4a~4h），其结构经¹H NMR、 ¹³C NMR和MS（ESI）表征。采用MTT法评价了化合物对白血病细胞（K562）、人肺癌细胞（A549）和人肝癌细胞（HepG2）的体外抑制活性。结果表明：N-N-(4-苄氧基-苯甲酰基)-O-二甲氨基丙基-L-酪氨酰基]-L-苯丙氨醇(4e)对HepG2和K542细胞的抑制活性均高于阳性对照药阿霉素，IC₅₀分别为0.41和11.77 μmol·L^-1。

Synthesis and Antitumor Activities of Novel L-tyrosine Dipeptide Derivatives

Nine novel L-tyrosine dipeptide derivatives(3b,4a^4h)were obtained by condensation reaction,hydrolysis and nucleophilic substitution reactions,using L-tyrosine methyl ester hydrochloride and 4-hydroxy-benzoicacid(PHBA)as starting material.The structures were characterized by 1 H NMR,13 C NMR and MS(ESI).In vitro anticancer activities against three human cancer cell lines(K562,A549 and HepG2)were demonstrated by MTT assays.The results showed that the inhibitory activity of compound 4e on HepG2 and K542 cells were better than the positive control drug doxorubicin,which IC 50 was 0.41 and 11.77μmol·L^-1,respectively.