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

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.