Novel mitochondria-targeted and fluorescent DNA alkylation agents with highly selective activity against cancer cells

Abstract A series of novel nitrogen mustard-based fluorescent compounds were reported with good mitochondrial targeting ability and DNA alkylation activity. The results indicated that these compounds can be used directly as reporting and imaging agents for gel electrophoresis and flow cytometry without the necessity of additional fluorescent tagging agents. Notably, the compound CXL92 displayed highly selective activity against lung cancer cell line A549 with an IC 50 value of 0.32 μM compared to normal cell (LO2).