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

• Published in: Sensors and actuators. B, Chemical Chemical, 2024-05, Vol.407, p.135454, Article 135454
• Main Authors: Yang, Chunmei, He, Pei, Meng, Qiuyu, Dong, Chune, Zhou, Hai-Bing, Yang, Lu
• Format: Article
• Language: English
• Subjects: Estrogen receptor; Live-cell 3D imaging; NIR fluorescent probes; Photostable probes; SERM
• ISSN: 0925-4005; 1873-3077
• DOI: 10.1016/j.snb.2024.135454

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)ylidene)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. [Display omitted] •A novel photostable NIR fluorescent probe TCFT was developed for estrogen receptor.•TCFT was successfully applied in prolong live-cell imaging of estrogen receptor by 3D confocal microscopy.•TCFT exhibited selective estrogen receptor modulator activity and potent antiproliferative activity for breast cancer therapy.•TCFT possessed the potential as a theranostic probe for estrogen receptor (+) breast cancer study.