Issue 61, 2017

Design, synthesis and biological evaluation of flavonoid salicylate derivatives as potential anti-tumor agents

Abstract

A series of flavonoid salicylate derivatives containing trimethoxybenzene and a series of chrysin salicylate derivatives were synthesized for use as anti-tumor agents, and evaluated for antiproliferative activity using three human tumor cells: MCF-7 (breast carcinoma cells), HepG2 (liver carcinoma cells), MGC-803 (gastric carcinoma cells) and the mice tumor cells MFC (forestomach carcinoma cells). A substituent group of a suitable size and the trimethoxybenzene had a certain influence on the bioactivity of the flavonoid salicylate derivatives. Compound 2 and its salicylate derivatives 7a–7g containing the trimethoxybenzene exhibited more antiproliferative activity. Among them, compound 7g displayed the most potent antiproliferative activity against MGC-803 cells and MFC cells with the concentration causing 50% inhibition of cell growth (IC50) values of 11.05 ± 1.58 μM and 13.73 ± 2.04 μM, respectively. The flow cytometry results showed that compound 7g caused the cell cycle to be arrested in the G0/G1 phase and induced apoptosis of MFC cells in a dose-dependent manner. Furthermore, compound 7g showed good anti-tumor activity in vivo. These results suggested that compound 7g could be a new, potent anti-tumor candidate which should be optimized and evaluated further.

Graphical abstract: Design, synthesis and biological evaluation of flavonoid salicylate derivatives as potential anti-tumor agents

Supplementary files

Article information

Article type
Paper
Submitted
30 Jun 2017
Accepted
20 Jul 2017
First published
03 Aug 2017
This article is Open Access
Creative Commons BY-NC license

RSC Adv., 2017,7, 38171-38178

Design, synthesis and biological evaluation of flavonoid salicylate derivatives as potential anti-tumor agents

X. Deng, Z. Wang, J. Liu, S. Xiong, R. Xiong, X. Cao, Y. Chen, X. Zheng and G. Tang, RSC Adv., 2017, 7, 38171 DOI: 10.1039/C7RA07235J

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