2. Academic Validation
  3. Design, synthesis and anticancer activity of novel nopinone-based thiosemicarbazone derivatives

Design, synthesis and anticancer activity of novel nopinone-based thiosemicarbazone derivatives

  • Bioorg Med Chem Lett. 2017 Jun 1;27(11):2360-2363. doi: 10.1016/j.bmcl.2017.04.024.
Yunyun Wang 1,  Wen Gu 2,  Yu Shan 3,  Fei Liu 3,  Xu Xu 2,  Yiqin Yang 4,  Qiangjian Zhang 1,  Yan Zhang 1,  Hongbo Kuang 1,  Zhonglong Wang 1,  Shifa Wang 5
Affiliations

Affiliations

  • 1 College of Chemical Engineering, Nanjing Forestry University, Nanjing, Jiangsu 210037, People's Republic of China.
  • 2 College of Chemical Engineering, Nanjing Forestry University, Nanjing, Jiangsu 210037, People's Republic of China; Jiangsu Key Lab of Biomass-based Green Fuels and Chemicals, Nanjing 210037, People's Republic of China.
  • 3 Institute of Botany, Jiangsu Province and Chinese Academy of Sciences (Nanjing Botanical Garden Mem.Sun Yat-Sen), 210014, People's Republic of China.
  • 4 Institute of Light Industry Science and Engineering, Nanjing Forestry University, Nanjing, Jiangsu 210037, People's Republic of China.
  • 5 College of Chemical Engineering, Nanjing Forestry University, Nanjing, Jiangsu 210037, People's Republic of China; Institute of Light Industry Science and Engineering, Nanjing Forestry University, Nanjing, Jiangsu 210037, People's Republic of China. Electronic address: wangshifa65@163.com.
PMID: 28431878 DOI: 10.1016/j.bmcl.2017.04.024
Abstract

A series of new nopinone-based thiosemicarbazone derivatives were designed and synthesized as potent Anticancer agents. All these compounds were identified by 1H NMR, 13C NMR, HR-MS spectra analyses. In the in vitro Anticancer activity, most derivatives showed considerable cytotoxic activity against three human Cancer cell lines (MDA-MB-231, SMMC-7721 and Hela). Among them, compound 4i exhibited most potent antitumor activity against three Cancer cell lines with the IC50 values of 2.79±0.38, 2.64±0.17 and 3.64±0.13μM, respectively. Furthermore, the cell cycle analysis indicated that compound 4i caused cell cycle arrest of MDA-MB-231 cells at G2/M phase. The Annexin V-FITC/7-AAD dual staining assay also revealed that compound 4i induced the early Apoptosis of MDA-MB-231 cells.

Keywords

Anticancer; Apoptosis; Nopinone; Thiosemicarbazone.

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