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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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

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

Volume 10, Issue 9, 2013

Page: [879 - 885] Pages: 7

DOI: 10.2174/15701808113109990009

Price: $65

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Abstract

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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