Abstract
A series of 3-chloro-4-(indol-3-yl)-2,5-pyrroledione derivatives were synthesized and evaluated for their cytotoxic activities in vitro against five human cancer cell lines (K562, A549, ECA-109, KB and SMMC-7721). Most compounds displayed potent cytotoxicity with IC50 values in low micromolar range. The results showed that the existence of the chlorine atom at 3-position on the pyrroledione ring was crucial for the activity. Compound 6a, the most potent one (IC50: 0.67∼3.93 μM), would be a promising template for further development of novel antitumor agents
Keywords: Antitumor, 3-Chloro-4-(indol-3-yl)-2, 5-pyrroledione, Cytotoxic activity, Heterocycles, Structure-activity relationship, Synthesis
Letters in Drug Design & Discovery
Title:Synthesis and Biological Evaluation of 3-Chloro-4-(indol-3-yl)-2,5- pyrroledione Derivatives as Antitumor Agents
Volume: 10 Issue: 5
Author(s): Yuchen Lin and Jing Chen
Affiliation:
Keywords: Antitumor, 3-Chloro-4-(indol-3-yl)-2, 5-pyrroledione, Cytotoxic activity, Heterocycles, Structure-activity relationship, Synthesis
Abstract: A series of 3-chloro-4-(indol-3-yl)-2,5-pyrroledione derivatives were synthesized and evaluated for their cytotoxic activities in vitro against five human cancer cell lines (K562, A549, ECA-109, KB and SMMC-7721). Most compounds displayed potent cytotoxicity with IC50 values in low micromolar range. The results showed that the existence of the chlorine atom at 3-position on the pyrroledione ring was crucial for the activity. Compound 6a, the most potent one (IC50: 0.67∼3.93 μM), would be a promising template for further development of novel antitumor agents
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Cite this article as:
Lin Yuchen and Chen Jing, Synthesis and Biological Evaluation of 3-Chloro-4-(indol-3-yl)-2,5- pyrroledione Derivatives as Antitumor Agents, Letters in Drug Design & Discovery 2013; 10 (5) . https://dx.doi.org/10.2174/1570180811310050003
DOI https://dx.doi.org/10.2174/1570180811310050003 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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