Chinese Journal of Organic Chemistry >
Synthesis and Antitumor Activity of Small Peptides Based on Phenylalanine Derivatives
Received date: 2015-05-04
Revised date: 2015-06-26
Online published: 2015-07-02
Supported by
Project supported by the National Natural Science Foundation of China (Nos. 21371052), the Heilongjiang Postdoctoral Scientific Research Foundation (No. LBH-Q14138) and the Scientific Research Fund of Heilongjiang Provincial Education Department (No. 12531512).
With the aim of obtaining potential antitumor candidates with more efficiency and more economic value, eight new small peptides based on phenylalanine derivatives were designed and synthesized. The target products were obtained via amino protection, amide condensation, amino deprotection, condensation, deprotection and condensation reactions with L-phenylalanine used as the starting material. The structures of target products are confirmed by FTIR, 1H NMR, I3C NMR, HRMS and elemental analysis. The antitumor activities of all target compounds are evaluated by thiazolyl blue tetrazolium bromide (MTT) method. The results showed that all compounds exhibited moderate antitumor activities against hepatoma carcinoma cell SMC7721. Compounds 5e and 8b exhibited the strongest inhibitory activities against hepatoma carcinoma cell, which could serve as lead compounds and provided valuable information for the further development of new antitumor agents.
Key words： phenylalanine; small peptide; antitumor activity tests; synthesis
Li Hongbao , Zhang Shuang , Gong Xianfeng , Hou Guangfeng , Yu Yinghui , Bai Youyin , Gao Jinsheng . Synthesis and Antitumor Activity of Small Peptides Based on Phenylalanine Derivatives[J]. Chinese Journal of Organic Chemistry, 2015 , 35(11) : 2429 -2436 . DOI: 10.6023/cjoc201505004
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