Synthesis and biological evaluation of novel 3,9-substituted β-carboline derivatives as anticancer agents

被引：23

作者：

Chen, Yi-Fong ^{[1
,2
,3
]}

Lin, Yi-Chien ^{[3
]}

Chen, Jeng-Pang ^{[3
]}

Chan, Hsu-Chin ^{[4
]}

Hsu, Mei-Hua ^{[3
]}

Lin, Hui-Yi ^{[3
]}

Kuo, Sheng-Chu ^{[1
,2
,3
]}

Huang, Li-Jiau ^{[1
,2
,3
]}

机构：

[1] China Med Univ, PhD Program Canc Biol & Drug Discovery, Taichung 40402, Taiwan

[2] Acad Sinica, Taichung 40402, Taiwan

[3] China Med Univ, Sch Pharm, Taichung 40402, Taiwan

[4] China Med Univ, Sch Med, Dept Biochem, Taichung 40402, Taiwan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2015年 / 25卷 / 18期

关键词：

beta-Carboline derivatives; Anticancer activity; Apoptosis; Structure-activity relationships (SARs); 1-Benzyl-3-(5-hydroxymethyl-2-furyl)indazole (YC-1) analogs; BENZODIAZEPINE RECEPTOR; APOPTOSIS; ANALOGS; ACTIVATION; ALKALOIDS; YC-1; CYTOTOXICITY; INHIBITION; HARMINE; PATHWAY;

D O I：

10.1016/j.bmcl.2015.07.058

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In our previous studies on 1-benzyl-3-(5-hydroxymethyl-2-furyl) indazole (YC-1) analogs, we synthesised numerous substituted carbazole and alpha-carboline derivatives, which exhibited anticancer activity. In this study, we designed and synthesised a series of 3,9-substituted beta-carbolines, by replacing the tricyclic rings of carbazole and alpha-carboline derivatives with isosteric beta-carboline, and evaluated anticancer activity. We observed that 9-(2-methoxybenzyl)-beta-carboline-3-carboxylic acid (11a) inhibited the growth of HL-60 cells by inducing apoptosis, with a half maximal inhibitory concentration of 4.0 mu M. Our findings indicate that b-carboline derivatives can be used as lead compounds for developing novel antitumor agents. (C) 2015 Elsevier Ltd. All rights reserved.

引用

页码：3873 / 3877

页数：5

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