β-咔啉衍生物的抗肿瘤及抗菌活性

Anti-tumor and Antimicrobial Activities of β-Carbolines

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.