Design, synthesis and bioactivity investigation of tetrandrine derivatives as potential anti-cancer agents

• DOI: 10.1039/c8md00125a
• Publication Date: 2018-05-04T13:04:24Z
• Authors: Junrong Song; Junjie Lan; Chao Chen; Shengcao Hu; Jialei Song; Wulin Liu; Xueyi Zeng; Huayong Lou; Yaacov Ben-David; Weidong Pan
• Keywords: Tetrandrine

Twenty-four 14-sulfonamide-tetrandrine derivatives as potential anti-cancer agents were synthesized. The synthetic investigated for their cytotoxic activity against human cancer cell lines MDA-MB-231, PC3, WM9, HEL and K562. Initially, the IC50 values (50% inhibitory concentrations) of all compounds determined. These exhibited potent, but distinct, effects on above-mentioned lines. Among them, compound 23, which was modified with a 2-naphthalenesulfonyl group at 14-amino position, showed impressive inhibition five lines, especially MDA-MB-231 cells an value 1.18 ± 0.14 μM. Further mechanism exploration that 23 induced potent apoptotic death in concentration-dependent manner. results revealed might be drug candidate.