Design, synthesis, and biological evaluation of novel PROTACs compounds with good ERα degradation ability.

• Tác giả: Xu Dong, Peihong Fan, Cheng Liu, Hongxiang Lou, Wengang Ren, Xueqian Yang, Tao Zhang, Jiaqing Zheng, Xiangnan Zheng
• Ngôn ngữ: eng
• Ký hiệu phân loại: 616.2004 Diseases of respiratory system
• Thông tin xuất bản: England : Bioorganic & medicinal chemistry , 2025
• Bộ sưu tập: NCBI
• ID: 695423

Tóm tắt

A series of ER-PROTACs compounds were designed, synthesized and tested for their ability to degrade estrogen receptor proteins and exhibit Human breast cancer cells (MCF-7) inhibition activity. Molecular docking simulations were performed using Discovery studio. Among these compounds, QDE-003-W had the highest estrogen receptor protein degradation ability and cellular activity, with a DC