Tertiary sulphonamide derivatives as dual acting small molecules that inhibit LSD1 and suppress tubulin polymerisation against liver cancer

A series of tertiary sulphonamide derivatives were synthesised and evaluated for their antiproliferative activity against liver cancer cell lines (SNU-475, HepG-2, Bel-7402). Among these sulphonamides, compound 17a displayed the best anti-liver Bel-7402 cells with an IC50 value 0.32 μM. Compound could effectively inhibit tubulin polymerisation 1.27 Meanwhile, it selectively suppressed LSD1 63 nM. It also concentration-dependently inhibited migration cells. Importantly, exhibited potent antitumor in vivo. All findings revealed that might be a sulphonamide-based dual inhibitor to treat cancer.