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

作　　者：李洪宝[1] 张爽[2] 龚显峰[1] 侯广峰[1,2] 于颖慧[1] 白有银 高金胜[1,2] 

机构地区：[1]黑龙江大学化学化工与材料学院,哈尔滨150080 [2]黑龙江大学农药工程中心,哈尔滨150080

出　　处：《有机化学》2015年第11期2429-2436,共8页Chinese Journal of Organic Chemistry

基　　金：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);黑龙江省教育厅科学研究基金(No.12531512)资助项目~~

摘　　要：为了寻找更高效、更经济的抗肿瘤药物,以L-苯丙氨酸为起始原料,经氨基保护、酰胺缩合、脱保护、再缩合、再脱保护、再缩合等多步反应,设计并合成了8种新型苯丙氨酸衍生物的小分子肽,并采用FTIR、1H NMR、I3C NMR、HRMS和元素分析等测试方法对其结构进行确认.采用溴化噻唑蓝四氮唑法(MTT)比色法对所有目标化合物进行了抗肿瘤活性测试,测试结果表明,所有化合物对肝癌细胞SMC7721均有一定的抑制作用,其中化合物5e和8b对肝癌细胞的抑制作用最强.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, I3 C 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.

关 键 词：苯丙氨酸 小分子肽 抗肿瘤活性测试 合成 

分 类 号：O629.72[理学—有机化学]