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

页码：674 / 680

页数：7

共 29 条

[21] 6-Hydroxy- and 6-methoxy-β-carbolines as acetyl- and butyrylcholinesterase inhibitors
Schott, Yvonne
Decker, Michael
Rommelspacher, Hans
Lehmann, Jochen
[J]. 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
Sun, Rongqin
Liu, Rui
Zhou, Chi
Ren, Zhenghua
Guo, Liang
Ma, Qin
Fan, Wenxi
Qiu, Liqin
Yu, Huijuan
Shao, Guang
Cao, Rihui
[J]. 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)
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.
[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2007, 17 (16) : 4657 - 4663
[24] Synthesis of neamine-carboline conjugates for RNA binding and their antibacterial activities
Wu, Shan
Fu, Yunsha
Yan, Ribai
Wu, Yanfen
Lei, Xiaoping
Ye, Xin-Shan
[J]. 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
Yang Jiajia
Wang Meng
Li Xia
Fan Ningning
Xue Liangmin
Li Hao
Tian Chao
Wang Xiaowei
Liu Junyi
Zhang Zhili
[J]. 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
Zhang Lan
Deng Xinshan
Wu Jiaofeng
Meng Guangpeng
Liu Congchong
Chen Guzhou
Zhao Qingchun
Hu Chun
[J]. 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
Zhu Huajie
Liu Li
Yang Qin
[J]. CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE, 2015, 36 (08): : 1559 - 1562

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