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
收稿日期: 2015-05-04
修回日期: 2015-06-26
网络出版日期: 2015-07-02
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
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).
李洪宝 , 张爽 , 龚显峰 , 侯广峰 , 于颖慧 , 白有银 , 高金胜 . 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[J]. 有机化学, 2015 , 35(11) : 2429 -2436 . DOI: 10.6023/cjoc201505004
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
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