2. Academic Validation
  3. Synthesis, in vitro cytotoxicity evaluation and mechanism of 5' monosubstituted chalcone derivatives as antitumor agents

Synthesis, in vitro cytotoxicity evaluation and mechanism of 5' monosubstituted chalcone derivatives as antitumor agents

  • Bioorg Med Chem Lett. 2023 Apr 1:85:129239. doi: 10.1016/j.bmcl.2023.129239.
Xueping Xu 1,  Jinjin Wang 1,  Baozhang Yan 2,  Yandong Leng 1,  Zhemin Chen 1,  Guojun Pan 3,  Cen Xiang 4,  Yuou Teng 5
Affiliations

Affiliations

  • 1 College of Sciences, Tianjin University of Science and Technology, Tianjin 300457, China.
  • 2 College of Sciences, Tianjin University of Science and Technology, Tianjin 300457, China; Jecho Biopharmaceuticals Co., Ltd, No.2633 ZhongBinDaDao, Tianjin Eco-City, Tianjin, China.
  • 3 College of Sciences, Tianjin University of Science and Technology, Tianjin 300457, China; Shandong First Medical University ＆ Shandong Academy of Medical Sciences, 271000, China.
  • 4 College of Sciences, Tianjin University of Science and Technology, Tianjin 300457, China. Electronic address: xiangcen@tust.edu.cn.
  • 5 College of Sciences, Tianjin University of Science and Technology, Tianjin 300457, China. Electronic address: tyo201485@tust.edu.cn.
PMID: 36924947 DOI: 10.1016/j.bmcl.2023.129239
Abstract

A series of 5' monosubstituted chalcone derivatives were synthesized to explore their antitumor activity and mechanism of action in vitro. The structures of 5' monosubstituted chalcone derivatives synthesized by reactions such as Suzuki coupling were confirmed by 1H NMR, 13C NMR and MS, and the target compounds were not reported in the literature. The antitumor activity of the aimed compounds was tested by MTT colorimetric method in vitro. Compound 5c has an IC50 value of 1.97 μM for K562 and a value of 2.23 μM for HepG2. Further investigation of the mechanism of action of compound 5c was found to have effects on K562 cell morphology, proliferation, Apoptosis, cell cycle, and wound healing of HepG2 cells. The results showed that compound 5c has research value in antitumor activity and mechanism of action in vitro.

Keywords

Chalcone derivatives; In vitro cytotoxicity; Mechanism of action.

Figures