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

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

Volume: 10 Issue: 9

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

Affiliation:

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

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.

Cite this article as:

Chen Jing, Du Wenting, Tao Xuefen, Huang Jiawei, Song Yuliang and Ying Huazhou, Synthesis and Biological Evaluation of Novel β-Carboline Derivatives as Antiproliferative Agents, Letters in Drug Design & Discovery 2013; 10 (9) . https://dx.doi.org/10.2174/15701808113109990009