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Selective and effective anticancer agents: Synthesis, biological evaluation and structure-activity relationships of novel carbazole derivatives

文献类型： 外文期刊

作者： Huang, Wenbo 1 ; Gao, Zilin 2 ; Zhang, Zhigang 1 ; Fang, Wei 1 ; Wang, Zuoqian 3 ; Wan, Zhongyi 1 ; Shi, Liqiao 1 ; Wang, 1 ;

作者机构： 1.Hubei Acad Agr Sci, Natl Biopesticide Engn Res Ctr, Hubei Biopesticide Engn Res Ctr, Wuhan 430064, Peoples R China

2.Huazhong Agr Univ, Coll Sci, Wuhan 430070, Peoples R China

3.Hubei Acad Agr Sci, Inst Plant Protect & Soil Sci, Wuhan 430064, Peoples R China

4.Minist Agr, Key Lab Integrated Pest Management Crops Cent Chi, Wuhan 430064, Peoples R China

关键词： Carbazole alkaloid; Analogues; Synthesis; Biological evaluation; Cytotoxic activity

期刊名称：BIOORGANIC CHEMISTRY （ 影响因子：5.275； 五年影响因子：5.252 ）

ISSN： 0045-2068

年卷期： 2021 年 113 卷

页码：

收录情况： SCI

摘要： Carbazole alkaloids is an important class of natural products with diverse biological functions. So, the aim of this article is to explore new chemical entities containing carbazole scaffold as potential novel cytotoxic agents based on our developed three-component indole-to-carbazole reaction. Two series of carbazole derivatives were designed and synthesized, and their in vitro cytotoxic activities against three cell lines (A875, HepG2, and MARC145) were evaluated. The results indicated that some of these carbazole derivatives exhibited significantly good cytotoxic activities against tested cell lines compared with the control 5-fluorouracil (5-FU). Especially, carbazole acylhydrazone compounds 7g and 7p displayed high inhibitory activity on cancer cells, but almost no activity on normal cells. Further analysis of induced apoptosis for potential compounds indicated that the potential antitumor agents induced cell death in A875 cells at least partly (initially) by apoptosis, which might be used as promising lead scaffold for discovery of novel carbazole-type cytotoxic agents.

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