Synthesis and bioactivities of novel dihydroartemisinin-piperazine derivatives containing sulfonamide.
- Author:
Chao MA
1
;
Xue-qiang LI
1
;
Jian XU
1
;
Cou-xi CHEN
1
Author Information
1. School of Chemistry and Chemical Engineering, Ningxia University, Yinchuan 750021, China.
- Publication Type:Journal Article
- MeSH:
Antineoplastic Agents;
chemical synthesis;
chemistry;
pharmacology;
Artemisinins;
chemical synthesis;
chemistry;
pharmacology;
Cell Proliferation;
drug effects;
HeLa Cells;
Humans;
Inhibitory Concentration 50;
Molecular Structure;
Piperazines;
chemical synthesis;
chemistry;
pharmacology;
Structure-Activity Relationship;
Sulfonamides;
chemistry
- From:
Acta Pharmaceutica Sinica
2013;48(9):1430-1435
- CountryChina
- Language:Chinese
-
Abstract:
Dihydroartemisinin is an important derivative of artemisinin. We used dihydroartemisinin as the starting material, through esterification, amination and acylation, a series of novel piperazine-sulfonamide contained dihydroartemisinin derivatives were firstly synthesized and their chemical structures were confirmed by IR, 1H NMR, 13C NMR and HR-MS. X-diffraction was used to determine the final configuration of the compound 3c. And the in vitro anti-HeLa activities of compounds 3 were analyzed with CCK-8 method. The preliminary bioassay test shows that compound 3 showed the best inhibition activities against HeLa with IC50 values of 0.14 micromol x L(-1).
