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

Abstract

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.

• Authors: Weihong Lai, Jiaxin Chen, Xinjiao Gao, Xiaobao Jin, Gong Chen, Lianbao Ye
• Journal: International journal of molecular sciences (Int J Mol Sci) Vol. 24 Issue 21 (Oct 25 2023) ISSN: 1422-0067 [Electronic] Switzerland
• PMID: 37958533 (Publication Type: Journal Article)

Chemical References

• Chalcone
• Chalcones
• Antineoplastic Agents
• Fluorouracil

Topics

• Humans
• Female
• Chalcone (pharmacology)
• Chalcones (pharmacology, therapeutic use)
• Structure-Activity Relationship
• Molecular Docking Simulation
• Cell Proliferation
• Drug Screening Assays, Antitumor
• Breast Neoplasms (drug therapy)
• Antineoplastic Agents (therapeutic use)
• Fluorouracil (pharmacology, therapeutic use)
• Molecular Structure
• Cell Line, Tumor