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.
- 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: [email protected].
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.