Anti-tumor and Antimicrobial Activities of β-Carbolines

被引:2
作者
Liu Li [1 ]
Ma Yangyang [2 ]
Wang Kuan [1 ]
Jia Yunjing [2 ]
Li Wan [2 ]
Zhu Huajie [2 ]
机构
[1] Hebei Univ, Coll Med, Baoding 071000, Peoples R China
[2] Hebei Univ, Coll Pharmaceut Sci, Baoding 071000, Peoples R China
来源
CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE | 2018年 / 39卷 / 04期
关键词
beta-Carboline; Antimicrobial activity; Anti-tumor activity; Chiral compound; ANTICANCER AGENTS; DERIVATIVES; DESIGN; INHIBITORS; BISCARBOLINE; BINDING; ACIDS;
D O I
10.7503/cjcu20170636
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
A series of beta-carbolines possessing different substituents at C1, C3 and N9 positions derived from L-tryptophan was used in anti-tumour and antimicrobial activity study. Compound 3b exhibited anti-tumour activity against tumour cell line A459 with a IC50 value of 3.17 mu mol/L in vitro by methyl thiazolyl tetrazolium(MTT) assay while the positive control group(cis-platin, DDP) was 1.45 mu mol/L. Other eleven compounds showed relatively weak activities against the five cell-lines. Compound 5h exhibited activitiy against vibrio anguillarum with a MIC value of 0.78 mu mol/L while the positive control group(ciprofloxacin) was 1.25 mu mol/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.
引用
收藏
页码:674 / 680
页数:7
相关论文
共 29 条
[21]   6-Hydroxy- and 6-methoxy-β-carbolines as acetyl- and butyrylcholinesterase inhibitors [J].
Schott, Yvonne ;
Decker, Michael ;
Rommelspacher, Hans ;
Lehmann, Jochen .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2006, 16 (22) :5840-5843
[22]   Synthesis and biological evaluation of piperazine group-linked bivalent β-carbolines as potential antitumor agents [J].
Sun, Rongqin ;
Liu, Rui ;
Zhou, Chi ;
Ren, Zhenghua ;
Guo, Liang ;
Ma, Qin ;
Fan, Wenxi ;
Qiu, Liqin ;
Yu, Huijuan ;
Shao, Guang ;
Cao, Rihui .
MEDCHEMCOMM, 2015, 6 (12) :2170-2174
[23]   Novel tetrahydro-β-carboline-1-carboxylic acids as inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2) [J].
Trujillo, John I. ;
Meyers, Marvin J. ;
Anderson, David R. ;
Hegde, Shridhar ;
Mahoney, Matthew W. ;
Vernier, William F. ;
Buchler, Ingrid P. ;
Wu, Kun K. ;
Yang, Syaluan ;
Hartmann, Susan J. ;
Reitz, David B. .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2007, 17 (16) :4657-4663
[24]   Synthesis of neamine-carboline conjugates for RNA binding and their antibacterial activities [J].
Wu, Shan ;
Fu, Yunsha ;
Yan, Ribai ;
Wu, Yanfen ;
Lei, Xiaoping ;
Ye, Xin-Shan .
TETRAHEDRON, 2010, 66 (19) :3433-3440
[25]   Syntheses and Antiproliferative Evaluation of 6-Thienyl, 6-Polyphenyl Aryl and 6-Naphthyl Derivatives of 2,4-Diaminopyrido [3,2-d]pyramidine as Non-classical Antifolate Targeting DHFR [J].
Yang Jiajia ;
Wang Meng ;
Li Xia ;
Fan Ningning ;
Xue Liangmin ;
Li Hao ;
Tian Chao ;
Wang Xiaowei ;
Liu Junyi ;
Zhang Zhili .
CHEMICAL RESEARCH IN CHINESE UNIVERSITIES, 2017, 33 (04) :559-568
[26]   Design, Synthesis and Biological Activities of N-(Furan-2-ylmethyl)-1H-indole-3-carboxamide Derivatives as Epidemal Growth Factor Receptor Inhibitors and Anticancer Agents [J].
Zhang Lan ;
Deng Xinshan ;
Wu Jiaofeng ;
Meng Guangpeng ;
Liu Congchong ;
Chen Guzhou ;
Zhao Qingchun ;
Hu Chun .
CHEMICAL RESEARCH IN CHINESE UNIVERSITIES, 2017, 33 (03) :365-372
[27]  
Zhu H. J., 2009, MODERN ORGANIC STERE, P283
[28]  
Zhu H. J., 2015, ORGANIC STEREOCHEMIS, P57
[29]   Vibrational Circular Dichroism in Study of Stereochemistry of Chiral β-Biscarboline with N-O Functional Group [J].
Zhu Huajie ;
Liu Li ;
Yang Qin .
CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE, 2015, 36 (08) :1559-1562