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

ID: ALA4368888

Journal: Medchemcomm

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

Authors: Xiong R, He D, Deng X, Liu J, Lei X, Xie Z, Cao X, Chen Y, Peng J, Tang G.

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.

CiteXplore: 31057737

DOI: 10.1039/C8MD00484F

Patent ID: ┄