A novel photostable near-infrared fluorescent selective estrogen receptor modulator (SERM) for live-cell 3D imaging of breast cancer

Estrogen receptor (ER) is a major transcriptional regulator that plays an important role in the treatment of breast cancer. Herein, we rationally designed and synthesized a novel small -molecule near -infrared (NIR) fluorescent probe, 2-(4-(2-(2,5-bis(2-fluoro-4-hydroxyphenyl)thiophen-3-yl)vinyl)- 3-cyano-5,5-dimethylfuran-2(5 H)yli- dene)malononitrile (TCFT), which could enable prolonged live -cell imaging by three-dimensional (3D) confocal microscopy. Moreover, this bifunctional probe also exhibited photostability, selective estrogen receptor modulator activity, and potent antiproliferative activity for targeted breast cancer therapy, which would be a prominent NIR fluorescent probe for breast cancer study.