2. Academic Validation
  3. Thiosemicarbazone-based selective proliferation inactivators inhibit gastric cancer cell growth, invasion, and migration

Thiosemicarbazone-based selective proliferation inactivators inhibit gastric cancer cell growth, invasion, and migration

  • Medchemcomm. 2017 Oct 23;8(12):2173-2180. doi: 10.1039/c7md00353f.
Biao Hu 1,  Bo Wang 1,  Bing Zhao 1,  Qian Guo 1,  Zhong-Hua Li 1,  Xin-Hui Zhang 1,  Guang-Yao Liu 1,  Ying Liu 1,  Ying Tang 1,  Fan Luo 1,  Ya Du 1,  Ya-Xin Chen 1,  Li-Ying Ma 1,  Hong-Min Liu 1
Affiliations

Affiliation

  • 1 Collaborative Innovation Center of New Drug Research and Safety Evaluation , Key Laboratory of Technology of Drug Preparation , Ministry of Education of China , School of Pharmaceutical Sciences , Zhengzhou University , Zhengzhou 450001 , Henan Province , PR China . Email: yingdejiqing1314@163.com ; Email: liuhm@zzu.edu.cn.
PMID: 30108734 DOI: 10.1039/c7md00353f
Abstract

A series of novel thiosemicarbazone derivatives were synthesized and evaluated for their antiproliferative activity against several selected tumor cell lines of different origins using the MTT assay. The preliminary results indicated that the MGC-803 cell line was remarkably sensitive to all the synthesized compounds. Among this series, compound 5n showed the best inhibitory activity with an IC50 value of 0.93 μM (about 10-fold more potent than 3-AP) against MGC-803. Further mechanism studies revealed that compound 5n could obviously inhibit the proliferation of MGC-803 cells by inducing Apoptosis and arresting the cell cycle at the S phase. Compound 5n also showed marked inhibition of cell migration and invasion, without significant cytotoxicity against gastric epithelial immortalized GES-1 cells.

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