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Targeting tumor acidic microenvironment, a cis-aconitate linked pyropheophorbide a dimer 3 was designed and prepared. The observed fluorescence quenching of 3 verified our FRET based molecular design. Acid-dependent cleavage in aqueous solution, singlet oxygen generation, and cytotoxicity against HepG2 cell lines of dimer 3 were investigated. The dimer demonstrated different levels of fluorescence recovery when incubated in acidic aqueous environment as well as effective phototoxicity against HepG2 cells.

Tumor Acidic Microenvironment Targeted Pyropheophorbide a Dimer, an Alternative Strategy for Simultaneous Tumor Fluorescence Imaging and PDT Treatment