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■ Synthesis and Biological Evaluation of 3-((1-Methyl-1H-pyrrol-2-yl)methylene)indolin-2-one Derivatives as Potent Anticancer Active Agents

Jie Chen, Wei-nan Hu, Yang Xu, Wen Li, Ya-yun Qi, Yi-hong Fu, Jia-min Liu, Zhen-chao Wang,* and Gui-ping Ouyang*

*College of Pharmacy, Guizhou University, Huaxi St., Guiyang 550025, China

Abstract

A series of 3-((1-methyl-1H-pyrrol-2-yl)methylene)indolin-2-one derivatives were designed, synthesized, and evaluated for their inhibition activities against four tumor cells in vitro. These compounds were fully characterized by 1H NMR, 13C NMR, and HRMS. Antitumor experiments indicated that some compounds exhibited significant inhibition activities against SMMC-7721. Especially, the IC50 values of 7k and 7l (IC50 = 8.08 ± 0.95 µM, IC50 = 3.01 ± 0.61 µM) demonstrated the best antitumor activities against SMMC-7721 (human hepatoma cell lines) than the positive agents Sunitinib (IC50 = 8.27 ± 0.40 µM). Likewise, their structure activity relationship (SAR) was studied.