2. Academic Validation
  3. Synthesis, cytotoxicity, and in vivo antitumor activity study of parthenolide semicarbazones and thiosemicarbazones

Synthesis, cytotoxicity, and in vivo antitumor activity study of parthenolide semicarbazones and thiosemicarbazones

  • Bioorg Med Chem. 2020 Jul 1;28(13):115557. doi: 10.1016/j.bmc.2020.115557.
Xinxin Jia 1,  Qi Liu 1,  Shiyi Wang 1,  Binglin Zeng 2,  Guohua Du 2,  Chen Zhang 3,  Yan Li 4
Affiliations

Affiliations

  • 1 School of Chemical Engineering, Beijing Institute of Petrochemical Technology, Beijing 102617, PR China.
  • 2 State Key Laboratory of Bioactive Substance and Function of Natural Medicines and Beijing Key Laboratory of Active Substances Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, PR China.
  • 3 School of Chemical Engineering, Beijing Institute of Petrochemical Technology, Beijing 102617, PR China; Beijing Key Laboratory of Enze Biomass Fine Chemicals, Beijing Institute of Petrochemical Technology, Beijing 102617, PR China. Electronic address: [email protected].
  • 4 State Key Laboratory of Bioactive Substance and Function of Natural Medicines and Beijing Key Laboratory of Active Substances Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, PR China. Electronic address: [email protected].
PMID: 32546298 DOI: 10.1016/j.bmc.2020.115557
Abstract

Parthenolide is an important sesquiterpene lactone with potent Anticancer activities. In order to further improve its biological activity, a series of parthenolide semicarbazone or thiosemicarbazone derivatives was synthesized and evaluated for their Anticancer activity. Derivatives were tested in vitro against 5 human tumor cell lines, and many of these showed higher cytotoxicity than parthenolide. Five compounds were further studied for their antitumor activity in mice. The in vivo result indicated that compound 4d showed both promising antitumor activity against mice colon tumor and small side effects on immune systems. The cell Apoptosis and cell cycle distribution of compound 4d were also studied. Molecular docking studies revealed multiple interactions between 4d and NF-κB. Our findings demonstrate the potential of semicarbazones as a promising type of compounds with Anticancer activity.

Keywords

Anticancer; In vivo; Parthenolide; Semicarbazone.

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