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Letters in Drug Design & Discovery


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

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

Author(s): Yuchen Lin and Jing Chen

Volume 10, Issue 5, 2013

Page: [382 - 389] Pages: 8

DOI: 10.2174/1570180811310050003

Price: $65


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

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