2. Academic Validation
  3. Design, synthesis and bioevaluation of novel prenylated chalcones derivatives as potential antitumor agents

Design, synthesis and bioevaluation of novel prenylated chalcones derivatives as potential antitumor agents

  • Eur J Pharm Sci. 2024 Jan 1:192:106660. doi: 10.1016/j.ejps.2023.106660.
Jia Yu 1,  Xia Wang 2,  Sha Cheng 1,  Xiaoping Zeng 1,  Xinwei Wan 1,  Shinan Wei 1,  Bixue Xu 1,  Heng Luo 3,  Xueling Meng 4
Affiliations

Affiliations

  • 1 State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Medical University, Guiyang, 550014, China; Natural Products Research Center of Guizhou Province, Guiyang, 550014, China.
  • 2 State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Medical University, Guiyang, 550014, China; Natural Products Research Center of Guizhou Province, Guiyang, 550014, China; Suiyang County Hospital of Traditional Chinese Medicine, Suiyang, 563300, China.
  • 3 State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Medical University, Guiyang, 550014, China; Natural Products Research Center of Guizhou Province, Guiyang, 550014, China. Electronic address: [email protected].
  • 4 State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Medical University, Guiyang, 550014, China; Natural Products Research Center of Guizhou Province, Guiyang, 550014, China. Electronic address: [email protected].
PMID: 38052256 DOI: 10.1016/j.ejps.2023.106660
Abstract

A series of novel prenylated chalcone derivatives with broad spectrum Anticancer potential were designed and synthesized. Some of the synthesized target compounds showed potent anti-proliferative activities toward LNCaP (prostate Cancer cell line), K562 (human leukemia cells), A549 (human lung carcinoma cell line) and HeLa (cervical Cancer cell line) cell lines. Among of the active compounds, (E)-1-(4-(2-(diethylamino)ethoxy)-2-hydroxy-6-methoxy-3-(3-methylbut-2-en-1-yl)phenyl)-3-(pyridin-3-yl)prop-2-en-1-one (C36) was directly interacted with protein kinase B (PKB), also known as Akt, significantly inhibited the pPI3K, pAKT(Ser473) protein levels to repress the growth of Cancer cells by inducing Apoptosis, arresting cell cycle. Our studies provide support for prenylated chalcone derivatives potential applications in Cancer treatment as a potential Akt Inhibitor.

Keywords

Antitumor; Cytotoxicity; PI3K/AKT pathway; Prenylated chalcone derivatives.

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