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Synthesis and Biological Evaluation of Novel β-Carboline Derivatives as Antiproliferative Agents
Jing Chen 1 #,Wenting Du 2 *,Xuefen Tao 3,Jiawei Huang 3,Yuliang Song 3
1.Department of Medicinal Chemistry, College of Pharmaceutical Science, Zhejiang Chinese Medicinal University, HangZhou 310053
2.Department of Pharmacy, Zhejiang Medical College, Hangzhou 310053, China
3.Department of Medicinal Chemistry, College of Pharmaceutical Science, Zhejiang Chinese Medicinal University, Hangzhou 310053, China
*Correspondence author
#Submitted by
Subject:
Funding: the Natural Science Foundation of China (No.No. 81102315, No. 21002016), Zhejiang Chinese Medicinal University Fundation (No.No. 751200F004), the Specialized Research Fund for the Doctoral Program of Higher Education of China (No.No. 20103322120002)
Opened online:12 July 2013
Accepted by: none
Citation: Jing Chen,Wenting Du,Xuefen Tao.Synthesis and Biological Evaluation of Novel β-Carboline Derivatives as Antiproliferative Agents[OL]. [12 July 2013] http://en.paper.edu.cn/en_releasepaper/content/4545993
 
 
A series of novel β-carboline derivatives were synthesized and evaluated for their cytotoxic activities in vitro against two human tumor cell lines. Many of the compounds showed moderate to potent cytotoxic activities against the tested cell lines, in which compound 12l exhibited the most potent antiproliferative activities against KB cell line (IC50 = 4.58 μM). Preliminary mechanism research on compound 12l indicated it could inhibit DNA intercalation and tubulin polymerization.
Keywords:Antiproliferative; Antitubulin; β-Carboline Derivatives; DNA intercalation; Structure-activity relationship; Synthesis
 
 
 

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