Design, synthesis and optimization of Apcin analogues as Cdc20 inhibitors for triple-negative breast cancer therapy.

• Tác giả: Shuyang Cao, Qingsong Chen, Zhuo Chen, Gaoyun Hu, Liqing Hu, Xiangyang Le, Qianbin Li, Qiwan Wen, Lei Zhang
• Ngôn ngữ: eng
• Thông tin xuất bản: France : European journal of medicinal chemistry , 2025
• Bộ sưu tập: NCBI
• ID: 733773

Tóm tắt

Cell division cycle 20 homologue (Cdc20) is an essential mitotic regulator whose overexpression is closely associated with tumorigenesis and poor prognosis in triple-negative breast cancer (TNBC). Targeting Cdc20 has therefore emerged as a promising therapeutic avenue for this aggressive malignancy. In the present study, a receptor-based drug design approach was employed to optimize Apcin analogues as Cdc20 inhibitors. Through a two-step strategy-concept validation followed by structural optimization-we identified compound 14c, which demonstrated remarkable Cdc20 binding affinity (K