Synthesis and Antitumor Activity of Small Peptides Based on Phenylalanine Derivatives

doi:10.6023/cjoc201505004

Chin. J. Org. Chem. ›› 2015, Vol. 35 ›› Issue (11): 2429-2436.DOI: 10.6023/cjoc201505004 Previous Articles Next Articles

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基于苯丙氨酸衍生物的小分子肽合成及抗肿瘤活性的研究

李洪宝^a, 张爽^b, 龚显峰^a, 侯广峰^a,b, 于颖慧^a, 白有银^a, 高金胜^a,b

a 黑龙江大学化学化工与材料学院哈尔滨 150080;
b 黑龙江大学农药工程中心哈尔滨 150080

收稿日期:2015-05-04 修回日期:2015-06-26 发布日期:2015-07-02
通讯作者: 侯广峰, 高金胜 E-mail:hougf@hlju.edu.cn;gaojins@hlju.edu.cn
基金资助:
国家自然科学基金(Nos. 21371052)、黑龙江省博士后科研启动基金(Nos. LBH-Q14138)及黑龙江省教育厅科学研究基金(No. 12531512)资助项目.

Synthesis and Antitumor Activity of Small Peptides Based on Phenylalanine Derivatives

Li Hongbao^a, Zhang Shuang^b, Gong Xianfeng^a, Hou Guangfeng^a,b, Yu Yinghui^a, Bai Youyin^a, Gao Jinsheng^a,b

a School of Chemistry and Materials Science, Heilongjiang University, Harbin 150080;
b Engineering Research Center of Pesticide, Heilongjiang University, Heilongjiang University, Harbin 150080

Received:2015-05-04 Revised:2015-06-26 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).

1. Synthesis and Antitumor Activity of Small Peptides Based on Phenylalanine Derivatives.PDF(2284KB)

Abstract

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

Cite this article

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]. Chin. J. Org. Chem., 2015, 35(11): 2429-2436.

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基于苯丙氨酸衍生物的小分子肽合成及抗肿瘤活性的研究

Synthesis and Antitumor Activity of Small Peptides Based on Phenylalanine Derivatives

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