Synthesis and Biological Evaluation of Novel β-Carboline Derivatives as Antiproliferative Agents

Author(s): Jing Chen, Wenting Du, Xuefen Tao, Jiawei Huang, Yuliang Song, Huazhou Ying.

Journal Name: Letters in Drug Design & Discovery

Volume 10 , Issue 9 , 2013

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A series of novel β-carboline derivatives was synthesized and evaluated for their cytotoxic activities in vitro against two human tumor cell lines. Most 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 that it could inhibit DNA intercalation and tubulin polymerization.

Keywords: Antiproliferative, Antitubulin, β-Carboline Derivatives, DNA intercalation, Structure-activity relationship, Synthesis.

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Article Details

Year: 2013
Page: [879 - 885]
Pages: 7
DOI: 10.2174/15701808113109990009
Price: $65

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