Citation: Liu Siyu, Dai Jiaojiao, You Jing, Wang Zhouyu, Yang Lingling. Syntheses and Anticancer Evaluations of Novel 3, 5-disubstituted-1H-indole Derivatives[J]. Chemistry, ;2018, 81(5): 456-460. shu

Syntheses and Anticancer Evaluations of Novel 3, 5-disubstituted-1H-indole Derivatives

College of Food and Bioengineering, Xihua University, Chengdu 610039

Corresponding author: Yang Lingling, yangll0808@sina.com
Received Date: 14 November 2017
Accepted Date: 16 March 2018

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Study on new anticancer drugs is one of the key tasks of global drug development. We previously found that 3, 5-disubstituted-1H-indole derivatives have apparent inhibitory activity against pancreatic cancer cells. Here we reported a new simple and efficient route for the synthesis of 3-((substituted-thio)methyl)-5-acylamino-1H-indole derivatives, which involves Vilsmeier-Haack reaction, Boc protection of secondary amine, aldehyde reduction, carboxylic acid and amine condensation reaction, and eight new target compounds (11a~11h) were synthesized. The cell-based assays revealed that 11a~11h have good inhibitory activity against pancreatic cancer cell line BxPC-3, and 11e is the most potent compound with an IC₅₀ value of 2.28μmol/L. 11e was observed to have no/low activity to other tested cancer cell lines and human normal liver cell line HL-7702, indicating that it is not a cytotoxic compound. Overall, 11e may be a good hit compound for further efforts to develop new inhibitors against pancreatic cancer.
- Tumour,
- Indole derivatives,
- Pancreatic cancer,
- Tumor cell
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