Design and synthesis of isatin/triazole conjugates that induce apoptosis and inhibit migration of MGC-803 cells

Eur J Med Chem. 2016 Nov 29:124:350-360. doi: 10.1016/j.ejmech.2016.08.065.

Bin Yu ¹, Sai-Qi Wang ², Ping-Ping Qi ², Dong-Xiao Yang ², Kai Tang ², Hong-Min Liu ³

Affiliations

1 School of Pharmaceutical Sciences & Collaborative Innovation Center of New Drug Research and Safety Evaluation, Zhengzhou University, Zhengzhou 450001, China. Electronic address: zzuyubin@hotmail.com.
2 School of Pharmaceutical Sciences & Collaborative Innovation Center of New Drug Research and Safety Evaluation, Zhengzhou University, Zhengzhou 450001, China.
3 School of Pharmaceutical Sciences & Collaborative Innovation Center of New Drug Research and Safety Evaluation, Zhengzhou University, Zhengzhou 450001, China. Electronic address: liuhm@zzu.edu.cn.

PMID: 27597411 DOI: 10.1016/j.ejmech.2016.08.065

Abstract

A series of new isatin/triazole conjugates were designed based on the hypothesis that the ester-linked compounds could be enzymatically hydrolyzed by cellular esterases inside the cells. These compounds showed moderate to good growth inhibition toward the tested Cancer cells, exerted selective inhibition toward MGC-803 cells and were less toxic to normal cells HL-7702 and GES-1. Of these compounds, compound 5a showed the best inhibitory activity against MGC-803 cells (IC₅₀ = 9.78 μM), induced Apoptosis through multiple mechanisms, as well as inhibited migration of MGC-803 cells.

Keywords

Apoptosis; Cytotoxicity; Isatin; LSD1 inactivation; Migration inhibition; Triazole.

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