Thiosemicarbazone-based selective proliferation inactivators inhibit gastric cancer cell growth, invasion, and migration†,RSC Medicinal Chemistry

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Thiosemicarbazone-based selective proliferation inactivators inhibit gastric cancer cell growth, invasion, and migration†
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2017-10-23 00:00:00 , DOI: 10.1039/c7md00353f
Biao Hu _{1,

2,

3,

4,

5} , Bo Wang _{1,

2,

3,

4,

5} , Bing Zhao _{1,

2,

3,

4,

5} , Qian Guo _{1,

2,

3,

4,

5} , Zhong-Hua Li _{1,

2,

3,

4,

5} , Xin-Hui Zhang _{1,

2,

3,

4,

5} , Guang-Yao Liu _{1,

2,

3,

4,

5} , Ying Liu _{1,

2,

3,

4,

5} , Ying Tang _{1,

2,

3,

4,

5} , Fan Luo _{1,

2,

3,

4,

5} , Ya Du _{1,

2,

3,

4,

5} , Ya-Xin Chen _{1,

2,

3,

4,

5} , Li-Ying Ma _{1,

2,

3,

4,

5} , Hong-Min Liu _{1,

2,

3,

4,

5}

Affiliation

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.

中文翻译：

基于硫氨基脲的选择性增殖灭活剂可抑制胃癌细胞的生长，侵袭和迁移†

合成了一系列新颖的硫代半碳酰胺衍生物，并使用MTT分析法评估了其对几种不同来源的选定肿瘤细胞系的抗增殖活性。初步结果表明，MGC-803细胞系对所有合成的化合物都非常敏感。在该系列中，化合物5n对MGC-803表现出最佳的抑制活性，IC ₅₀值为0.93μM（比3-AP强约10倍）。进一步的机理研究表明，化合物5n可以通过诱导细胞凋亡并使细胞周期停留在S期而明显抑制MGC-803细胞的增殖。复合5n 还显示出对细胞迁移和侵袭的显着抑制，而对胃上皮永生化GES-1细胞没有明显的细胞毒性。

更新日期：2017-10-23

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