β-咔啉衍生物的抗肿瘤及抗菌活性  

Anti-tumor and Antimicrobial Activities of β-Carbolines

作　　者：刘莉 马洋洋 王宽 贾云静 李婉 朱华结[2] LIU Li;MA Yangyang;WANG Kuan;JIA Yunjing;LI Wan;ZHU Huajie(College of Medicine, 2. College of Pharmaceutical Sciences, Hebei University, Baoding 071000, China)

机构地区：[1]河北大学医学院,保定071000 [2]河北大学药学院,保定071000

出　　处：《高等学校化学学报》2018年第4期674-680,共7页Chemical Journal of Chinese Universities

基　　金：河北省教育厅科研项目(批准号:QN2017021);河北大学"一省一校"专项项目(批准号:2017030)资助~~

摘　　要：以L-色氨酸为原料合成了72个不同取代基的β-咔啉化合物,其中31个新化合物,包括12对手性化合物.采用噻唑蓝(MTT)法对5种肿瘤细胞株及5种菌株进行了体外抗肿瘤活性、抗菌活性的筛选及构效关系研究.生物活性测试结果表明,部分目标化合物具有一定的抗肿瘤活性(化合物3b对A549细胞的IC_(50)=3.17μmol/L),且具有不同程度的抑菌活性(化合物5h对鳗弧菌的MIC=0.78μmol/L).A series of β-carbolines possessing different substituents at C1,C3 and N9 positions derived from L-tryptophan was used in anti-tumour and antimicrobial activity study. Compound 3 b exhibited anti-tumour activity against tumour cell line A459 with a IC50 value of 3. 17 μmol/L in vitro by methyl thiazolyl tetrazolium（ MTT） assay while the positive control group（ cis-platin,DDP） was 1. 45 μmol/L. Other eleven compounds showed relatively weak activities against the five cell-lines. Compound 5 h exhibited activitiy against vibrio anguillarum with a MIC value of 0. 78 μmol/L while the positive control group（ ciprofloxacin） was 1. 25μmol/L. Other fourteen compounds showed relatively weak activities against five spices of bacteria. By the study of structural-activity relationship,optimizing structures is possible and necessary in the future to screen potential compounds for medicinal study.

关 键 词：β-咔啉化合物 抗菌活性 抗肿瘤活性 手性化合物 

分 类 号：O626[理学—有机化学]