Design and Synthesis of Novel Chalcone Derivatives: Anti-Breast Cancer Activity Evaluation and Docking Study

Authors：Lai, Weihong; Chen, Jiaxin; Gao, Xinjiao; Jin, Xiaobao; Chen, Gong^*; Ye, Lianbao^*

Source：INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES, 2023, 24(21): 15549.

DOI：10.3390/ijms242115549

• chalcones
• synthesis
• anti-breast cancer (MCF-7)
• molecular docking

Chalcone is a common simple fragment of natural products with anticancer activity. In a previous study, the research group discovered a series of chalcone derivatives with stronger anticancer activities. To find better anticancer drugs, novel chalcone derivatives A1-A14, B1-B14 have continuously been designed and synthesized. The antiproliferative activity of these compounds against breast cancer cells (MCF-7) was investigated by the Cell Counting Kit-8 (CCK-8) method with 5-fluorouracil (5-Fu) as the control drug. The results showed that compound A14 exhibited excellent antiproliferative ability compared to the control drug 5-Fu. Scratch experiments and cloning experiments further confirmed that compound A14 could inhibit the proliferation and colony formation activity of MCF-7 cells. In addition, molecular docking primarily explains the interaction between compound and protein. These results suggested that compound A14 could be a promising chalcone derivative for further anti-breast cancer research.

• Institution
  广东药学院