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中文摘要：
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（MTr）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。
英文摘要：
OBJECTIVE To explore the synthesis of novel phenylalanine dipeptide derivatives and their inhibitory effects on tumor cells. METHODS Starting from L-phenylalanine or L-tyrosine, a series of derivatives were synthesized by reaction with chloroacetyl chloride, follo~ved by condensation with L-phenylalaninol or L-phenylalanine methyl ester hydrochloride and nucleophilic substitution reaction with differently substituted phenol. The cell proliferation inhibiting activities of the derivatives were evaluated by thiazolyl blue tetrazolium bromide（MTY） method. RESULTS Some of the target compounds showed certain inhibitory effect for leukemia cell lines I（562 and HEL in vitro. Furthermore, the derivatives 3f and 3q had preferably inhibitory effect on K562 cell line prostate cancer PC3 cells in vitro. CONCLUSION Phenylalanine dipeptide derivatives possess good effect on the leukemia and prostate cancer cells and are worth of further research.
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