Synthesis and Biological Evaluation of 3-Chloro-4-(indol-3-yl)-2,5- pyrroledione Derivatives as Antitumor Agents

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 (IC_50: 0.67∼3.93 μM), would be a promising template for further development of novel antitumor agents

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