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

Related Articles

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

Bioorg Med Chem Lett. 2017 Apr 09;:

Authors: Wang Y, Gu W, Shan Y, Liu F, Xu X, Yang Y, Zhang Q, Zhang Y, Kuang H, Wang Z, Wang S

Abstract
A series of new nopinone-based thiosemicarbazone derivatives were designed and synthesized as potent anticancer agents. All these compounds were identified by (1)H NMR, (13)C 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.

PMID: 28431878 [PubMed - as supplied by publisher]

http://ift.tt/2oAXtNa