A Photoactivatable AIEgen for Selective Imaging and Killing of Estrogen Receptor-Positive Cells

The development of fluorescent probes based on the skeletal structure of small-molecule targeted anticancer drugs is promising for biomedical applications because these probes generally show trackable fluorescence and connatural bioactivity inherited from the parental anticancer drugs. By mimicking a classic estrogen receptor (ER) antagonist, namely, tamoxifen, we herein design and synthesize a photoactivatable luminogen with aggregation-induced emission and medicinal benefits. The probe is weakly emissive when it is selectively internalized by estrogen receptor-positive cells. Under photoirradiation, its emission can be turned on to report the intracellular distribution. The cell viability assay suggests that the probe only exhibits cytotoxicity to ER-positive cells but negligible cytotoxicity to ER-negative cells. This study thus provides new access to targeted theranostic systems with photoactivity.