Журнал "Макрогетероциклы"

Lei Cao,^a Shisheng Wang,^a Liu Wang,^a Xiuhan Guo,^a Guangzhe Li,^a and Weijie Zhao^a,b@ 

^aSchool of Pharmaceutical Science and Technology, Dalian University of Technology, 116024 Dalian, P.R. China

^bState Key Laboratory of Fine Chemicals, Dalian University of Technology, 116024 Dalian, P.R. China

^@Corresponding author E-mail: zyzhao@dlut.edu.cn; pharmscizhao@163.com

DOI: 10.6060/mhc190336z

Macroheterocycles 2019 12(2) 187-192

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.