Design, synthesis and mechanism studies of dual EZH2/BRD4 inhibitors for cancer therapy

Xinye Chen,Cheng Wang,Dehua Lu,Heng Luo,Shang Li,Fucheng Yin,Zhongwen Luo,Ningjie Cui,Lingyi Kong,Xiaobing Wang

Bioorganic & Medicinal Chemistry（2023）

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Abstract

•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.

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Key words

Solid tumor,EZH2,BRD4,SAR

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