Synthesis and anti-tumor activities of L-phenylalanine dipeptide derivatives
- Author:
Lei HU
1
Author Information
- Publication Type:Journal Article
- Keywords: Anti-tumor activity; Derivatives; Phenylalanine dipeptide; Synthesis
- From: Chinese Pharmaceutical Journal 2016;51(21):1831-1838
- CountryChina
- Language:Chinese
- Abstract: 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, followed 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(MTT) method. RESULTS: Some of the target compounds showed certain inhibitory effect for leukemia cell lines K562 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.
