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目的探索苯丙氨酸二肽的合成及对肿瘤细胞的抑制作用。方法以L-苯丙氨酸、4-硝基-L-苯丙氨酸或L-酪氨酸为原料经酰化、缩合、亲核取代等反应,设计合成苯丙氨酸二肽衍生物,并用噻唑蓝(MTT)法评价了目标化合物对5种肿瘤细胞株的生长抑制活性。结果合成了17个目标化合物,体外活性显示,部分化合物对白血病细胞株K562、HEL具有一定的抑制作用,衍生物3f、3q对K562细胞株及前列腺癌细胞株PC3有较好的抑制作用。结论苯丙氨酸二肽衍生物对抑制白血病及前列腺肿瘤细胞具有较好的抑制作用,具有进一步研究的价值。
Objective To explore the synthesis of phenylalanine dipeptide and its inhibitory effect on tumor cells. Methods The reaction of L-phenylalanine, 4-nitro-L-phenylalanine or L-tyrosine with acylation, condensation and nucleophilic substitution was designed to synthesize phenylalanine dipeptide derivatives , And the growth inhibitory activity of the target compounds on five tumor cell lines was evaluated by MTT assay. Results 17 target compounds were synthesized. In vitro activity of some compounds showed some inhibitory effects on leukemia cell line K562 and HEL. The derivatives 3f and 3q showed good inhibitory effect on K562 cell line and PC3 cell line. Conclusion Phenylalanine dipeptide derivatives have good inhibitory effect on the inhibition of leukemia and prostate tumor cells, which has the value of further research.