L-苯丙氨酸二肽衍生物的合成及其抗肿瘤活性研究

Synthesis and Anti-tumor Activities of L-Phenylalanine Dipeptide Derivatives

目的:探讨L-苯丙氨酸二肽衍生物的合成及其抗肿瘤活性。方法:以L-酪氨酸或L-苯丙氨酸为原料,依次酰化反应、缩合反应、亲核取代及烷基化等反应合成得到苯丙氨酸二肽衍生物,并用噻唑蓝(MTT)法测定其对人前列腺癌细胞(PC3)、人慢性髓原白血病细胞(K562)、人红白细胞白血病细胞(HEL)3类肿瘤细胞株的抗肿瘤活性。结果:共合成了3a^3h共8个未见文献报道的苯丙氨酸二肽衍生物,MTT结果显示,部分衍生物对K562细胞株具有一定抑制作用,衍生物3b,3e,3f对PC3和K562有较好的抑制作用。结论:合成了8个新的苯丙氨酸二肽衍生物,其对K562及PC3肿瘤细胞株具有一定的抑制作用。

Objective： To synthesize L-phenylalanine dipeptide derivatives and study their inhibitory effects on tumor cells. Methods： Starting from L-tyrosine or L-phenylalanine,L-phenylalanine dipeptide derivatives were synthesized via acetylation,condensation,nucleophilic substitution and/or alkylation. The cell proliferation inhibiting activities of the derivatives were evaluated by thiazolyl blue tetrazolium bromide（ MTT） method. Results： A total of 8 3 a - 3 h phenylalanine dipeptide derivatives were synthesized. Some of the target compounds showed certain inhibitory effect against leukemia cell lines K562 and HEL in vitro. Furthermore,the derivatives 3 b,3 e and 3 f had preferably inhibitory effect on prostate cancer cell line PC3 and K562 cells in vitro. Conclusions： Phenylalanine dipeptide derivatives possess good inhibitory effects on the leukemia and prostate cancer cells and are worth of further research.