Bioactivity and application of phenoxazines with different mitochondria-targeted lipophilic cationic groups.

Mitochondria have been recognized as a significant target for cancer therapy due to their vital role in many basic cell functions. In recent years, the development of mitochondrial targeted anti-tumor drugs has become important research directions. Herein, We report three new targeted preparations (FEQ-TPP, FEQ-BDP, and FEQ-TEA), which were synthesized by conjugating triphenylphosphine (TPP), Bodipy-pyridine salt (BDP) and triethylamine salt (TEA) with phenoxazine (FEQ). It was observed that greater delocalization range of TPP cationic carriers can enhance the recognition and accumulation efficiency of FEQ-TPP in tumor cell mitochondria. As a result, FEQ-TPP exhibits excellent mitochondrial targeting and significant anti-tumor selectivity; FEQ-BDP can show the ability of real-time fluorescence imaging. This research provides valuable insights for the screening of mitochondrial targeting vectors and the subsequent exploration and development of targeted anti-tumor medications, particularly those based on phenoxazine and its derivatives. [Display omitted] • FEQ-TPP demonstrated remarkable antitumor selectivity. • FEQ-BDP showed real-time fluorescence imaging and excellent mitochondrial targeting ability. • Different lipophilic cations have different effects. [ABSTRACT FROM AUTHOR]