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Design, synthesis and biological evaluation of tryptamine salicylic acid derivatives as potential antitumor agents

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Abstract

A series of tryptamine salicylic acid derivatives were synthesized and their antiproliferative activity against MGC-803, MCF-7, HepG2, A549 and HeLa cell lines was evaluated. The structure–activity relationship (SAR) study revealed that different substitutions of the C5 and C3′–C5′ positions have certain effects on the anti-proliferation activity. The growth assay revealed that N-[2-(5-bromo-1H-indol-3-yl)-ethyl]-2-hydroxy-3-methyl-benzamide (E20) showed the most potent and broad-spectrum anticancer inhibition of all the cell lines evaluated, and was only more potent than 5-Fu for the gastric cancer cell line. Preliminary studies indicated that compound E20 could inhibit colony formation and migration of MGC-803 cells. The flow cytometry (FCM) results showed that compound E20 arrested the cell cycle in the G2/M phase and induced apoptosis of MGC-803 cells in a concentration-dependent manner. In addition, the western blot results showed that E20 can down-regulate the expression of hexokinase 2. Our studies suggest that the framework of N-[2-(5-bromo-1H-indol-3-yl)-ethyl]-2-hydroxy-3-methyl-benzamide may be consider as a new type of chemical for designing effective anti-cancer drugs targeting gastric cancer cells.

Graphical abstract: Design, synthesis and biological evaluation of tryptamine salicylic acid derivatives as potential antitumor agents

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Publication details

The article was received on 27 Sep 2018, accepted on 05 Jan 2019 and first published on 11 Jan 2019


Article type: Research Article
DOI: 10.1039/C8MD00484F
Citation: Med. Chem. Commun., 2019, Advance Article

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    Design, synthesis and biological evaluation of tryptamine salicylic acid derivatives as potential antitumor agents

    R. Xiong, D. He, X. Deng, J. Liu, X. Lei, Z. Xie, X. Cao, Y. Chen, J. Peng and G. Tang, Med. Chem. Commun., 2019, Advance Article , DOI: 10.1039/C8MD00484F

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