Thiosemicarbazone-based selective proliferation inactivators inhibit gastric cancer cell growth, invasion, and migration

Abstract

A series of novel thiosemicarbazone derivatives were synthesized and evaluated for their antiproliferative activity against several selected tumor cell lines of different origins using the MTT assay. The preliminary results indicated that the MGC-803 cell line was remarkably sensitive to all the synthesized compounds. Among this series, compound <b>5n</b> showed the best inhibitory activity with an IC₅₀ value of 0.93 μM (about 10-fold more potent than <b>3-AP</b>) against MGC-803. Further mechanism studies revealed that compound <b>5n</b> could obviously inhibit the proliferation of MGC-803 cells by inducing apoptosis and arresting the cell cycle at the S phase. Compound <b>5n</b> also showed marked inhibition of cell migration and invasion, without significant cytotoxicity against gastric epithelial immortalized GES-1 cells.