Novel mitochondria-targeted, nitrogen mustard-based DNA alkylation agents with near infrared fluorescence emission

In this report, the design of two novel nitrogen mustard-based DNA cross-linking agents with fluorophores incorporated into the structure (TN-A and TN-B) is disclosed. The results indicate that TN-A and TN-B can serve directly as both reporting and imaging agents for flow cytometry and gel electrophoresis without the necessity of another fluorescent tagging agents. TN-A and TN-B both selectively locate in the mitochondria and exhibit good antitumor activity. Notably, TN-A is the first DNA crosslinking agent with near infrared fluorescence emission properties.