Design, synthesis and mechanism studies of dual EZH2/BRD4 inhibitors for cancer therapy
Bioorganic & Medicinal Chemistry(2023)
摘要
•A series of dual inhibitors targeting EZH2 and BRD4 have been designed, synthesized, and evaluated.•KWCX-28 exhibited BRD4 inhibitory activity and the activity of binding to EZH2.•KWCX-28 exhibited potent inhibitory activity against HCT-116 cells.•BRD4 related proteins were detected in EZH2Is GSK126-administered group.
更多查看译文
关键词
Solid tumor,EZH2,BRD4,SAR
AI 理解论文
溯源树
样例
生成溯源树,研究论文发展脉络
Chat Paper
正在生成论文摘要