Citation: TAN Xuxia, LI Shining, ZHAO Jie, MAO Shen, MAO Longfei, XU Guiqing. Synthesis and Antitumor Activity of Novel 4H-1,2,4-Benzothiadiazine 1,1-Dioxide Derivatives[J]. Chinese Journal of Applied Chemistry, ;2016, 33(9): 1067-1072. doi: 10.11944/j.issn.1000-0518.2016.09.150420 shu

Synthesis and Antitumor Activity of Novel 4H-1,2,4-Benzothiadiazine 1,1-Dioxide Derivatives

TAN Xuxia ^a ,
LI Shining ^a ,
ZHAO Jie ^b ,
MAO Shen ^a ,
MAO Longfei ^a ,
XU Guiqing ^a,,

1.
a School of Chemistry and Chemical Engineering, He'nan Normal university, Xinxiang, He'nan 453007, China;
2.
b Topfond Pharmaceutical Limited by Share Ltd, Zhumadian, He'nan 463000, China

Corresponding author: XU Guiqing,
Received Date: 30 November 2015
Available Online: 24 March 2016
Fund Project:

Twelve unreported 4H-1,2,4-benzothiadiazine 1,1-dioxide derivatives were synthesized from 2-nitrobenzene sulfonyl chloride with good water-solubility in high yields. These compounds were characterized by ¹H NMR, ¹³C NMR, MS-ESI and elemental analysis. Their inhibiting effects on HepG-2 cell were evaluated with MTT protocol. The results show that 7-(aminomethyl)-3-cyclopropyl-1,1-dioxide-4H-benzo[e] [1,2,4]thiadiazine(7c) exhibits the highest inhibition rate of 79.3% among the synthesized compounds.
- 4H-benzothiadiazine dioxides derivatives,
- synthesis,
- antitumor activities
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