A novel nitrogen mustard functionalized tripodal AIE compound act as prodrug for fluorescent imaging and anticancer

The detection and treatment of cancer is a very important and challenging subject. Herein, the conception of aggregation-induced emission (AIE) is introduced into the design of anticancer drugs. A novel nitrogen mustard functionalized tripodal AIE anticancer prodrug (TM) was designed and synthesized. Interestingly, the TM had strong fluorescent in DMSO/H2O (water fraction 50%) binary solution. The fluorescence experiments showed that TM could enter the nucleus and cytoplasm of HepG2 cells. The TM could be used for both fluorescent imaging and killing cancer cells. The in vitro cytotoxicity of TM was about 3.2 fold than that of the free nitrogen mustard against HepG2 cells. This related to the unique design improved the effective content of nitrogen mustard drugs. The design that introduced AIE into anticancer drugs provides a effective approach to the detection and treatment of cancer.