Synthesis and bioactivities of novel dihydroartemisinin-piperazine derivatives containing sulfonamide / 药学学报
Acta Pharmaceutica Sinica
; (12): 1430-1435, 2013.
Article
in Zh
| WPRIM
| ID: wpr-259458
Responsible library:
WPRO
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).
Full text:
1
Index:
WPRIM
Main subject:
Pharmacology
/
Piperazines
/
Structure-Activity Relationship
/
Sulfonamides
/
HeLa Cells
/
Molecular Structure
/
Chemistry
/
Inhibitory Concentration 50
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Artemisinins
/
Cell Proliferation
Limits:
Humans
Language:
Zh
Journal:
Acta Pharmaceutica Sinica
Year:
2013
Type:
Article